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Journal articles on the topic 'Improved Systemic Bioavailability'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Tan, Sui Ling Janet, and Nashiru Billa. "Improved Bioavailability of Poorly Soluble Drugs through Gastrointestinal Muco-Adhesion of Lipid Nanoparticles." Pharmaceutics 13, no. 11 (2021): 1817. http://dx.doi.org/10.3390/pharmaceutics13111817.

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Gastrointestinal absorption remains indispensable in the systemic delivery of most drugs, even though it presents several challenges that, paradoxically, may also provide opportunities that can be exploited to achieve maximal bioavailability. Drug delivery systems made from nanoparticle carriers and especially, lipid carriers, have the potential to traverse gastrointestinal barriers and deploy in the lymphatic pathway, which aptly, is free from first pass via the liver. Several poorly soluble drugs have presented improved systemic bioavailability when couriered in lipid nanoparticle carriers.

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Hossain, Khondker Rufaka, Amani Alghalayini, and Stella M. Valenzuela. "Current Challenges and Opportunities for Improved Cannabidiol Solubility." International Journal of Molecular Sciences 24, no. 19 (2023): 14514. http://dx.doi.org/10.3390/ijms241914514.

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Cannabidiol (CBD), derived from the cannabis plant, has gained significant attention due to its potential therapeutic benefits. However, one of the challenges associated with CBD administration is its low bioavailability, which refers to the fraction of an administered dose that reaches systemic circulation. This limitation necessitates the exploration of various approaches to enhance the bioavailability of CBD, thus helping to maximize its therapeutic potential. A variety of approaches are now emerging, including nanoemulsion-based systems, lipid-based formulations, prodrugs, nanocarriers, an

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Het, Patel*, Patel Jaini, Ghanshyam Patel Dr., Yadav Priyanka, and Divykant Patel Dr. "REVIEW-SUBLINGUAL ROUTE FOR SYSTEMIC DRUG DELIVERY." World Journal of Pharmaceutical Science and Research 2, no. 2 (2023): 45–57. https://doi.org/10.5281/zenodo.10894235.

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Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a rapid onset of action and better patient compliance than orally ingested tablets. Sublingual literally meaning is “under the tongue”, administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability. Sublingual technology is convenient for dosing in ger

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Kim, Hyeongmin, Jong Hyuk Lee, Jee Eun Kim, et al. "Micro-/nano-sized delivery systems of ginsenosides for improved systemic bioavailability." Journal of Ginseng Research 42, no. 3 (2018): 361–69. http://dx.doi.org/10.1016/j.jgr.2017.12.003.

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5

Pawar, Poonam P., Hemant S. Ghorpade, and Bhavana A. Kokane. "Sublingual route for systemic drug delivery." Journal of Drug Delivery and Therapeutics 8, no. 6-s (2018): 340–43. http://dx.doi.org/10.22270/jddt.v8i6-s.2097.

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Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a rapid onset of action and better patient compliance than orally ingested tablets. Sublingual literally meaning is “under the tongue”, administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability. Sublingual technology is convenient for dosing in geriatric, pedi

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6

Rashid, Mamunur, Mohd Yaseen Malik, Sandeep K. Singh, Swati Chaturvedi, Jiaur R. Gayen, and Muhammad Wahajuddin. "Bioavailability Enhancement of Poorly Soluble Drugs: The Holy Grail in Pharma Industry." Current Pharmaceutical Design 25, no. 9 (2019): 987–1020. http://dx.doi.org/10.2174/1381612825666190130110653.

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Background: Bioavailability, one of the prime pharmacokinetic properties of a drug, is defined as the fraction of an administered dose of unchanged drug that reaches the systemic circulation and is used to describe the systemic availability of a drug. Bioavailability assessment is imperative in order to demonstrate whether the drug attains the desirable systemic exposure for effective therapy. In recent years, bioavailability has become the subject of importance in drug discovery and development studies. Methods: A systematic literature review in the field of bioavailability and the approaches

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Nilwani, Krutika S., Hemalata Wadkar, Aishwarya R. Ghanwat, and Shital P. Narwade. "A Review on In-Situ Nasal Gel." International Journal of Research and Review 12, no. 1 (2025): 603–11. https://doi.org/10.52403/ijrr.20250168.

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In situ gelling drug delivery techniques have garnered a lot of interest in the last ten years. When exposed to a range of endogenous stimuli, such as temperature increases, pH shifts, and the presence of ions, they can gel from their sol-state prior to injection. Systems can be given in a number of ways to facilitate the injection of a local or systemic treatment. They can also be used as efficient carriers for drug-carrying nanoparticles and microparticles. either natural, synthetic, or combined with a semi-artificial polymer that exhibits in situ gelling activity. In order to extend the tim

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8

Dubashynskaya, Natallia V., and Yury A. Skorik. "Patches as Polymeric Systems for Improved Delivery of Topical Corticosteroids: Advances and Future Perspectives." International Journal of Molecular Sciences 23, no. 21 (2022): 12980. http://dx.doi.org/10.3390/ijms232112980.

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Mucoadhesive polymer patches are a promising alternative for prolonged and controlled delivery of topical corticosteroids (CS) to improve their biopharmaceutical properties (mainly increasing local bioavailability and reducing systemic toxicity). The main biopharmaceutical advantages of patches compared to traditional oral dosage forms are their excellent bioadhesive properties and their increased drug residence time, modified and unidirectional drug release, improved local bioavailability and safety profile, additional pain receptor protection, and patient friendliness. This review describes

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9

Rachamalla, Hari Krishnareddy, Santanu Bhattacharya, Ajaz Ahmad, et al. "Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery." Nanomedicine 16, no. 8 (2021): 641–56. http://dx.doi.org/10.2217/nnm-2020-0470.

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Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of

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Sharma, Ankit, Avinash Kumar Gupta, Manish Kumar Gupta, and Vijay Sharma. "A Review: Formulation and Characterization of Fast Dissolving Tablet of Carvidilol." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 749–52. http://dx.doi.org/10.22270/jddt.v9i3.2738.

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Carvedilol a poorly water soluble drug undergoes extensive first pass metabolism, which reduces its bioavailability to 25-30%. Fast dissolving tablets of Carvedilol were prepared with the purpose of delivering the drug directly into the systemic circulation and bypassing the hepatic first pass metabolism with a concomitant increase in bioavailability. The solubility of Carvedilol was improved by forming inclusion complex with cyclodextrin which was then further used for the formulation of Fast dissolving tablet. Keywords: Carvedilol, Superdisintegrats, Fast dissolving Tablets and FDTs.

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11

Li, Qiang, Jun Cao, Qi Wang, et al. "Nanomized tumor-microenvironment-active NIR fluorescent prodrug for ensuring synchronous occurrences of drug release and fluorescence tracing." Journal of Materials Chemistry B 7, no. 9 (2019): 1503–9. http://dx.doi.org/10.1039/c8tb03188f.

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A nanomized NIR fluorescent prodrug was developed with improved bioavailability and tumor-targeting ability. Nanomized tumor-microenvironment-active NIR DCM-S-GEM/PEG prodrug provides a novel approach to realize long real-time tracking of drug delivery and activation process without systemic toxicity in vivo.

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12

Lakavath, Sunil Kumar. "Novel Delivery System Used for Oral Bioavailability Enhancement of Poorly Water Soluble Drugs." Journal of Drug Delivery and Therapeutics 10, no. 6-s (2020): 139–44. http://dx.doi.org/10.22270/jddt.v10i6-s.4613.

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Majority of the drugs used for the treatment of various diseases are administered by oral route using conventional delivery. The major drawback of the oral administration is the poor bioavailability due to the poor water solubility, chemical stability and pre-systemic metabolism. Numerous researches are going on for the improvement of oral bioavailability of drugs using novel drug delivery systems as an alternative to conventional delivery systems. Majority of the novel delivery system includes; solid dispersion, sustained, controlled buccal, gastro retentive, nano carrier delivery systems suc

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13

Zakir, Foziyah, Adil Ahmad, Uzma Farooq, et al. "Design and development of a commercially viable in situ nanoemulgel for the treatment of postmenopausal osteoporosis." Nanomedicine 15, no. 12 (2020): 1167–87. http://dx.doi.org/10.2217/nnm-2020-0079.

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Aim: To investigate the potential of a thermosensitive intranasal formulation of raloxifene hydrochloride (RH) for systemic delivery with the possibility of enhanced bioavailability and anti-osteoporotic efficacy. Methods: In this work, a commercially scalable nanoemulsion in thermosensitive gel, aligned with better clinical acceptability, has been developed and evaluated. Results: A significant 7.4-fold improvement in bioavailability of RH was recorded when compared with marketed tablets. Likewise, in vivo pharmacodynamics studies suggested 162% enhanced bone density and significantly improve

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14

Deleanu, Mariana, Laura Toma, Gabriela Maria Sanda, et al. "Formulation of Phytosomes with Extracts of Ginger Rhizomes and Rosehips with Improved Bioavailability, Antioxidant and Anti-Inflammatory Effects In Vivo." Pharmaceutics 15, no. 4 (2023): 1066. http://dx.doi.org/10.3390/pharmaceutics15041066.

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The poor water solubility of natural antioxidants restricts their bioavailability and therapeutic use. We aimed to develop a new phytosome formulation with active compounds from extracts of ginger (GINex) and rosehips (ROSAex) designed to increase their bioavailability, antioxidant and anti-inflammatory properties. The phytosomes (PHYTOGINROSA-PGR) were prepared from freeze-dried GINex, ROSAex and phosphatidylcholine (PC) in different mass ratios using the thin-layer hydration method. PGR was characterized for structure, size, zeta potential, and encapsulation efficiency. Results showed that P

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15

Patel, Sweta, Shruti Chopra, Simran Chaurasia, and Maryam Sarwat. "Plant based Bioavailability Enhancers." Current Pharmaceutical Design 28, no. 8 (2022): 642–54. http://dx.doi.org/10.2174/1381612828666220112141355.

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Abstract: Many of the synthetic and herbal drugs, despite their notable in vitro findings, demonstrate insignificant in vivo activity, the majority of the time due to poor bioavailability. As per Biopharmaceutical Classification System (BCS), one of the main concerns is low solubility and/or permeation of drugs resulting in reduced absorption and poor bioavailability. To overcome these issues, various strategies have been adopted, including the use of permeation enhancers which are also known as bioenhancers. Bioenhancers are synthetic or natural compounds that increase the bioavailability of

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16

Bučević Popović, Viljemka, Esma Karahmet Farhat, Ines Banjari, Antonia Jeličić Kadić, and Livia Puljak. "Bioavailability of Oral Curcumin in Systematic Reviews: A Methodological Study." Pharmaceuticals 17, no. 2 (2024): 164. http://dx.doi.org/10.3390/ph17020164.

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Curcumin is a natural compound found in turmeric that exhibits diverse biological activities. However, its poor bioavailability limits its therapeutic application, which has led to the development of various bioavailability-improved formulations. In this methodological study, we analyzed whether systematic reviews on curcumin considered the bioavailability of systemic oral curcumin formulations when synthesizing evidence from human clinical trials. A total of 171 systematic reviews published between 2003 and 2022 were included in the study. From the included studies, we extracted data on study

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17

Ogba, Chukwuemeka Emmanuel, Akpabio Elijah Akwaowoh, Ifeoluwa Adetomiwa Taiwo, Precious Joshua Edem, and Sunday Olajide Awofisayo. "Optimizing levofloxacin delivery using nanoparticles: a strategy for improved bioavailability and targeted release." Journal of Drug Delivery and Therapeutics 15, no. 5 (2025): 42–49. https://doi.org/10.22270/jddt.v15i5.7119.

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Nanoparticle-based drug delivery systems have emerged as a powerful strategy to enhance drug bioavailability and ensure targeted therapeutic release. Levofloxacin (LFX), a widely used broad-spectrum fluoroquinolone antibiotic, is limited by poor aqueous solubility, low oral bioavailability, and systemic side effects. This study investigates the formulation, characterization, and evaluation of levofloxacin-loaded nanoparticles aimed at improving its pharmacological performance. Various nanoparticle carriers, including polymeric nanoparticles, lipid-based nanocarriers, and inorganic nanoparticle

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18

Bácskay, Ildikó, Petra Arany, Pálma Fehér, et al. "Bioavailability Enhancement and Formulation Technologies of Oral Mucosal Dosage Forms: A Review." Pharmaceutics 17, no. 2 (2025): 148. https://doi.org/10.3390/pharmaceutics17020148.

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The oral mucosa is a versatile surface for drug administration, supporting both local and systemic therapies. Many active substances are effectively absorbed in the oral cavity, offering an alternative to enteral administration by bypassing the harsh gastrointestinal environment and hepatic first-pass metabolism. This has made oral mucosal drug delivery a growing area of research. Enhancing the bioavailability of active ingredients is a key focus in pharmaceutical technology, especially given the challenges of developing new drugs. Numerous strategies to improve bioavailability are compatible

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19

Gurav, Sonali, Anshu Sharma, Sunita Shinde, and Raju Rathod. "Polymeric Nanoparticles in Oncology: Design, Development and Characterization." Journal of Neonatal Surgery 14, no. 15S (2025): 615–37. https://doi.org/10.63682/jns.v14i15s.3547.

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Non-small cell lung cancer (NSCLC) treatment is often limited by the poor aqueous solubility and systemic side effects of Erlotinib, an EGFR inhibitor. To overcome these challenges, this study explores the use of β-Cyclodextrin (BCD), a natural polymer, for the development of biodegradable polymeric nanoparticles to enhance drug solubility, bioavailability, and therapeutic efficacy. Erlotinib-loaded BCD-based nanoparticles were formulated using High-Pressure Homogenization (HPH) and characterized for particle size, polydispersity index (PDI), zeta potential, drug encapsulation efficiency, and

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20

Vidhyalakshmi, R. Kowsika M. Pratheeba G. Blessy Flarance T. Punithavalli S. Dr. K. Rajaganapathy* Dr. R. Srinivasan. "Exploring the Use of Lipid-based Formulations for Improved Solubility of Hydrophobic Drugs." International Journal of Pharmaceutical Sciences 3, no. 1 (2025): 682–716. https://doi.org/10.5281/zenodo.14628636.

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Lipid-based formulations (LBFs) have emerged as a promising strategy for improving the solubility and bioavailability of hydrophobic drugs, which face absorption challenges due to poor water solubility. By utilizing lipid carriers such as emulsions, solid lipid nanoparticles, and liposomes, these formulations enhance drug dissolution and permeability in the gastrointestinal tract. LBFs can bypass first-pass metabolism through lymphatic transport, increasing systemic availability. Additionally, they offer protective encapsulation and sustained drug release, making them highly versatile in thera

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21

Ewuzie, Somtochukwu R., Calistus D. Nwakile, Emmanuel M. Uronnachi, et al. "Oral Gentamicin Sulphate Nanoemulsion for Systemic Indication: Formulation and Evaluation." Asian Journal of Research in Medical and Pharmaceutical Sciences 13, no. 3 (2024): 129–39. http://dx.doi.org/10.9734/ajrimps/2024/v13i3268.

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Aim: To achieve systemic availability of an oral dosage form of gentamicin sulfate (GS), typically impermeable via the gastrointestinal tract. Study Design: Formulation and physical characterization of GS nanoemulsion. Stability studies and ex vivo bioavailability evaluation of the emulsion. Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University Awka, Anambra State, Nigeria; between January 2021 and May 2023. Methodology: Pre-formulation experiments were conducted with adjuvants for use for the formu

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Ankita, Padale1 Ajit Tuwar2 Dr. Megha Salve3. "Transdermal Drug Delivery Systems: A Non-Invasive Approach to Medication Administration." International Journal of Pharmaceutical Sciences 2, no. 11 (2024): 1165–71. https://doi.org/10.5281/zenodo.14211648.

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Transdermal drug delivery systems (TDDS) are non-invasive, self-contained dosage forms designed to deliver therapeutic agents through the skin and into the systemic circulation. TDDS offer a valuable alternative to oral and injectable routes, providing improved patient compliance, reduced side effects, and sustained drug release. These systems utilize various technologies, including patches, gels, and sprays, to facilitate drug permeation across the skin barrier. Key benefits of TDDS include: Enhanced bioavailability Reduced first-pass metabolism Prolonged drug action Minimized systemic side e

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Tiwari, Sandip B., and Mansoor M. Amiji. "Improved Oral Delivery of Paclitaxel Following Administration in Nanoemulsion Formulations." Journal of Nanoscience and Nanotechnology 6, no. 9 (2006): 3215–21. http://dx.doi.org/10.1166/jnn.2006.440.

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Nanoemulsion formulations were designed for enhancing the oral bioavailability of hydrophobic drugs. Paclitaxel was selected as a model hydrophobic drug, which is also a substrate for the P-glycoprotein efflux system. The oil-in-water (o/w) nanoemulsions were formulated with pine nut oil as the internal oil phase, egg lecithin as the primary emulsifier, and water as the external phase. Stearylamine and deoxycholic acid were used to impart positive and negative charge to the emulsions, respectively. Nanoemulsions were prepared by sonication method and characterized for particle size and surface

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Fuentes-Rios, David, Alvaro Sanchez-Rodriguez, Laura Lopez-Rios, et al. "Human Pharmacokinetic Profiling and Comparative Analysis of Mangiferin and Its Monosodium Derivative from Mangifera indica Extracts Using UHPLC-MS/MS with 1H NMR and MALDI-TOF Confirmation." Molecules 30, no. 3 (2025): 461. https://doi.org/10.3390/molecules30030461.

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Mangiferin, a glucosyl xanthone, is a plant metabolite with promising nootropic and ergogenic properties. However, its poor and inconsistent systemic bioavailability limits its therapeutic potential. Additionally, the pharmacokinetics of mangiferin from mango leaf extract formulations remain uncharacterized in humans. This study validated a UHPLC-MS/MS method and conducted a human pharmacokinetic study approved by an ethics committee. The bioavailability of mangiferin and its monosodium salt was assessed from two standardized mango leaf extracts: MLE60, standardized to 60% mangiferin but pract

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Alfei, Silvana, and Guendalina Zuccari. "Attempts to Improve Lipophilic Drugs’ Solubility and Bioavailability: A Focus on Fenretinide." Pharmaceutics 16, no. 5 (2024): 579. http://dx.doi.org/10.3390/pharmaceutics16050579.

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The development of numerous drugs is often arrested at clinical testing stages, due to their unfavorable biopharmaceutical characteristics. It is the case of fenretinide (4-HPR), a second-generation retinoid, that demonstrated promising in vitro cytotoxic activity against several cancer cell lines. Unfortunately, response rates in early clinical trials with 4-HPR did not confirm the in vitro findings, mainly due to the low bioavailability of the oral capsular formulation that was initially developed. Capsular 4-HPR provided variable and insufficient drug plasma levels attributable to the high

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Omer, Safaa, and Romána Zelkó. "A Systematic Review of Drug-Loaded Electrospun Nanofiber-Based Ophthalmic Inserts." Pharmaceutics 13, no. 10 (2021): 1637. http://dx.doi.org/10.3390/pharmaceutics13101637.

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Currently, ocular inserts and nanoparticles have received much attention due to the limited bioavailability of conventional eye preparations and the toxicity problems of systemic drug administration. The current systematic review aims to present recent studies on the use of electrospun nanofiber-based ocular inserts to improve the bioavailability of drugs used for different ophthalmic diseases. A systematic search was performed in PubMed, Ovid Medline, Web of Science, ScienceDirect, Scopus, Reaxys, Google Scholar, and Google Patents/Espacenet taking “drug-loaded”, “nanofibers”, and “ophthalmic

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Trombino, Sonia, Roberta Cassano, Maria Luisa Di Gioia, and Francesca Aiello. "Emerging Trends in Green Extraction Techniques, Chemical Modifications, and Drug Delivery Systems for Resveratrol." Antioxidants 14, no. 6 (2025): 654. https://doi.org/10.3390/antiox14060654.

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Resveratrol is a naturally occurring phytoalexin found in red grapes, cocoa berries, and red grape wine. This compound exhibits potent antioxidant, anti-inflammatory, and anticancer properties. However, its clinical application is significantly hindered by poor aqueous solubility and rapid degradation at physiological pH, resulting in extremely low systemic bioavailability. This review explores three key aspects: green extraction methods for the efficient and sustainable isolation of resveratrol; structure–activity relationship studies of resveratrol derivatives to identify compounds with impr

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Gupta, Sakshi, ,. Archana, and Abadhesh Kumar Niranjan. "A Comprehensive Review on In-Situ Gel Drug Delivery System." Journal of Drug Delivery and Therapeutics 12, no. 4-S (2022): 245–48. http://dx.doi.org/10.22270/jddt.v12i4-s.5539.

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Over the past ten years, in situ gelling drug delivery methods have attracted a lot of attention. Prior to injection, they are in a sol-state, and they can gel when exposed to a variety of endogenous stimuli, including temperature rise, pH changes, and the presence of ions. Such to accomplish the injection of a local or systemic medication, systems may be delivered by a variety of can also be employed effectively as carriers for nano- and microparticles that carry drugs. Natural or artificial or in conjunction with semi-artificial polymer exhibiting in situ gelling behaviour. For the developme

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Tapas, Kumar Mohapatra* Sayed Razaur Raheman Abhijit Sahu Shruti Naik Rajesh Pothal. "Microspheres As Innovative Carriers for Controlled and Targeted Drug Delivery." International Journal of Pharmaceutical Sciences 3, no. 6 (2025): 77–92. https://doi.org/10.5281/zenodo.15569854.

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In pharmaceutical formulations, controlled drug delivery methods have become increasingly sophisticated during the last three decades. Microsphere is one of the best controlled drug delivery systems. One of the most promising and adaptable drug delivery technologies, microspheres provide a number of benefits for delivering therapeutic substances in a targeted and sustained manner. These spherical, biodegradable carriers can encapsulate a variety of medications, such as proteins, peptides, and tiny compounds. They are usually made with natural or synthetic polymers. Microspheres' controlled rel

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Ciullo, Alessandra, Vanessa Biemmi, Giuseppina Milano, et al. "Exosomal Expression of CXCR4 Targets Cardioprotective Vesicles to Myocardial Infarction and Improves Outcome after Systemic Administration." International Journal of Molecular Sciences 20, no. 3 (2019): 468. http://dx.doi.org/10.3390/ijms20030468.

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Cell therapy has been evaluated to enhance heart function after injury. Delivered cells mostly act via paracrine mechanisms, including secreted growth factors, cytokines, and vesicles, such as exosomes (Exo). Intramyocardial injection of cardiac-resident progenitor cells (CPC)-derived Exo reduced scarring and improved cardiac function after myocardial infarction in rats. Here, we explore a clinically relevant approach to enhance the homing process to cardiomyocytes (CM), which is crucial for therapeutic efficacy upon systemic delivery of Exo. By overexpressing exosomal CXCR4, we increased the

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Rutuja, Jadhav* Aadinath Sangle Dr. Megha Salve. "Buccal Films: Revolutionizing Oral Drug Delivery through Enhanced Bioavailability and Patient Compliance." International Journal of Pharmaceutical Sciences 2, no. 11 (2024): 1097–111. https://doi.org/10.5281/zenodo.14210586.

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Buccal films have transformed oral drug delivery, offering enhanced bioavailability, rapid absorption, and improved patient compliance. The oral cavity’s mucosal membrane presents an attractive route for systemic and local therapy, leveraging the ease of administration and patient-centric benefits of oro-mucosal drug delivery. This comprehensive review discusses – Benefits and drawbacks of buccal drug delivery, Anatomical and physiological aspects of oral mucosa,  In vitro techniques for examining buccal drug delivery systems, Key excipients are highlighted, including- Polymer

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Kij, Agnieszka, Anna Bar, Kamil Przyborowski, et al. "Thrombin Inhibition Prevents Endothelial Dysfunction and Reverses 20-HETE Overproduction without Affecting Blood Pressure in Angiotensin II-Induced Hypertension in Mice." International Journal of Molecular Sciences 22, no. 16 (2021): 8664. http://dx.doi.org/10.3390/ijms22168664.

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Angiotensin II (Ang II) induces hypertension and endothelial dysfunction, but the involvement of thrombin in these responses is not clear. Here, we assessed the effects of the inhibition of thrombin activity by dabigatran on Ang II-induced hypertension and endothelial dysfunction in mice with a particular focus on NO- and 20-HETE-dependent pathways. As expected, dabigatran administration significantly delayed thrombin generation (CAT assay) in Ang II-treated hypertensive mice, and interestingly, it prevented endothelial dysfunction development, but it did not affect elevated blood pressure nor

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Paul, Moumita, Pintu Sarkar, Riyanka Sengupta та ін. "Enhancement of solubility of Metaclopramide using solid dispersion technique with different carriers (HPβCD, PVP K-30)". Journal of Drug Delivery and Therapeutics 9, № 6 (2019): 17–22. http://dx.doi.org/10.22270/jddt.v9i6.3663.

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Modern drug discovery has led to the development of drug molecules that exhibit high lipophilicity and poor water solubility, which leads to problematic bioavailability. Approaches have thus been made to enhance dissolution of poorly water soluble drugs through modifications and creation of specific formulations. Metaclopramide is an antiemetic and gastroprokinetic agent, commonly used to treat nausea and vomiting. It is absorbed well after oral administration but a significant first pass effect in some human patients may reduce systemic bioavailability to 30%.The Metaclopramide base is thus m

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Deshmukh, Amol S., Kundan J. Tiwari, and Vijay R. Mahajan. "Solubility Enhancement Techniques for Poorly Water-Soluble Drugs." International Journal of Pharmaceutical Sciences and Nanotechnology 10, no. 3 (2017): 3701–8. http://dx.doi.org/10.37285/ijpsn.2017.10.3.1.

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Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for optimum pharmacological response. Poorly water-soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Poor aqueous solubility is a major problem encountered with formulation development of new chemical entities. There are over 40% of new chemical entities that exhibit poor solubility and low bioavailability. As per BCS clas

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T.M., Venugopal, Saroj Yadav, Madhuri Bhushan Patil, et al. "Nanoformulation of Phytochemicals to Increase Antifungal Effectiveness Against Pathogens Resistant to Drugs." Journal of Neonatal Surgery 14, no. 10S (2025): 479–87. https://doi.org/10.52783/jns.v14.2861.

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Introduction: Drug resistance, a lack of effective alternatives, and systemic toxicity are major problems when it comes to treating fungal infections with traditional antifungal medications. Because of its low solubility and bioavailability, the bioactive chemical curcumin, which possesses antifungal and anti-inflammatory characteristics, has restricted therapeutic value. The use of lipid nanoparticles shows promise as a means to improve targeted therapy, bioavailability, and medication delivery. Using the bioactive characteristics of curcumin to improve therapeutic effectiveness while reducin

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Gonzalez, Daniel, and Hartmut Derendorf. "Ciclesonide in the Management of Asthma." Clinical Medicine. Therapeutics 1 (January 2009): CMT.S2133. http://dx.doi.org/10.4137/cmt.s2133.

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Ciclesonide is a novel inhaled corticosteroid (ICSs) approved in most countries for the management of persistent asthma. Although inhaled corticosteroids are first-line therapy in the treatment of asthma, long term use and high-doses of these products may result in significant side effects. When developing a new ICSs, the goal is to identify a drug with comparable (or superior) efficacy to active comparators, and an improved safety profile. Ciclesonide is a prodrug which is administered through a hydrofluoroalkane-propellant metered dose inhaler (HFA-MDI). Once it reaches the lungs, the parent

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Anam Adil, Fida Muhammad, Qasim Ishtiaq, Sana Rashid, and Hunza Rashid. "Lipid-based Nanoparticles as Oral Drug Delivery Platforms for Overcoming Gastrointestinal Absorption Barriers and Enhancing the Bioavailability of Peptide- and Protein-based Therapeutics." Indus Journal of Bioscience Research 3, no. 5 (2025): 13–23. https://doi.org/10.70749/ijbr.v3i5.1255.

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The oral delivery and formulation of therapeutic peptide- and protein-based biopharmaceuticals continue to pose significant challenges within the pharmaceutical domain. These biomolecules exhibit inherently low oral bioavailability, primarily due to limited gastrointestinal solubility and permeability. Contributing factors include high molecular weight, poor membrane permeability, and extensive degradation by chemical and enzymatic processes within the gastrointestinal tract, all of which restrict their therapeutic potential. This review critically examines the barriers associated with oral ad

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Tabanelli, Rita, Simone Brogi, and Vincenzo Calderone. "Improving Curcumin Bioavailability: Current Strategies and Future Perspectives." Pharmaceutics 13, no. 10 (2021): 1715. http://dx.doi.org/10.3390/pharmaceutics13101715.

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Curcumin possesses a plethora of interesting pharmacological effects. Unfortunately, it is also characterized by problematic drug delivery and scarce bioavailability, representing the main problem related to the use of this compound. Poor absorption, fast metabolism, and rapid systemic clearance are the most important factors contributing to low curcumin levels in plasma and tissues. Accordingly, to overcome these issues, numerous strategies have been proposed and are investigated in this article. Due to advances in the drug delivery field, we describe here the most promising strategies for in

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Pires, Patrícia C., Ana Cláudia Paiva-Santos, and Francisco Veiga. "Nano and Microemulsions for the Treatment of Depressive and Anxiety Disorders: An Efficient Approach to Improve Solubility, Brain Bioavailability and Therapeutic Efficacy." Pharmaceutics 14, no. 12 (2022): 2825. http://dx.doi.org/10.3390/pharmaceutics14122825.

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Most drugs used for the treatment of depression, anxiety and related disorders have low absorption, high metabolism, low brain targeting and/or low water solubility, which can make it hard to formulate them at high strength and can also lead to decreased bioavailability. Incorporating these drugs into nanometric emulsions can solve these issues. Hence, the aim of the present review was to assess the potential of nano and micro emulsions for the delivery of antidepressant and anxiolytic drugs. The results from several studies showed that nanometric emulsions were able to increase drug strength

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Khatri, Upasana, Sunil Saini, and Meenakshi Bharkatiya. "Pharmaceutical Considerations of Nasal In-Situ Gel As A Drug Delivery System." Asian Journal of Pharmaceutical Research and Development 9, no. 3 (2021): 94–103. http://dx.doi.org/10.22270/ajprd.v9i3.950.

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In situ gelling drug delivery systems have gained enormous attention over the last decade. They are in a sol-state before administration, and they are capable of forming gels in response to different endogenous stimuli, such as temperature increase, pH change and the presence of ions. Such systems can be administered through different routes, to achieve local or systemic drug delivery and can also be successfully used as vehicles for drug-loaded nano- and microparticles. Natural, synthetic and/or semi-synthetic polymers with in situ gelling behaviour can be used alone, or in combination, for t

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Zulcaif, Nadiah Zafar, Asif Mahmood, Rai Muhammad Sarfraz, and Abdelhamid Elaissari. "Simvastatin Loaded Dissolvable Microneedle Patches with Improved Pharmacokinetic Performance." Micromachines 13, no. 8 (2022): 1304. http://dx.doi.org/10.3390/mi13081304.

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Microneedle patches (MNPs) are one of the emerging approaches for drug delivery involving minimal invasion and improved skin penetration of macro- and micro-entities. Herein, we report dissolvable microneedle patches (dMNPs) as a novel tool for better systemic delivery of Simvastatin in the management of hypocholesteremia. Thiolated chitosan (TC), polyvinyl pyrolidone (PVP) and polyvinyl alcohol (PVA) were employed in the development of dMNPs. Developed patches were characterized through SEM, FTIR, DSC, TGA, PXRD, dissolution testing, tensile strength, elongation (%), skin irritation studies,

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Kim, Min-Hwan, Dong Hyun Kim, Duy-Thuc Nguyen, et al. "Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib." Pharmaceutics 12, no. 8 (2020): 718. http://dx.doi.org/10.3390/pharmaceutics12080718.

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PEGylated Eudragit L100 (ELP)-containing proliponiosomes (PLNs) were developed for improved oral delivery of celecoxib (CXB). The successful introduction of PEG 2000 or 5000 to Eudragit L100 (EL) was confirmed via proton nuclear magnetic resonance analysis of which calculated molar substitution ratio of PEG to EL was 36.0 or 36.7, respectively. CXB, ELP, phospholipid, and non-ionic surfactants were dissolved in dimethyl sulfoxide and lyophilized to produce CXB-loaded PLNs (CXB@PLNs). The physical state of CXB@PLNs was evaluated using differential scanning calorimetry and powder X-ray diffracto

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Kirk, Christopher J., Monette A. Aujay, Mark Ho, et al. "Pharmacologic Evaluation of Orally Bioavailable Inhibitors of the 20S Proteasome." Blood 108, no. 11 (2006): 3581. http://dx.doi.org/10.1182/blood.v108.11.3581.3581.

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Abstract Clinical application of proteasome inhibitors in the treatment of hematologic malignancies such as myeloma and lymphoma is restricted in part by the necessity of frequent IV administration and would be improved by oral (PO) administration. Selective inhibitors of the protease subunits of the 20S proteasome can be generated from peptidyl aldehydes, boronates, vinyl sulfones, and epoxyketones. Many of these peptide based proteasome inhibitors are cell permeant and capable of systemic proteasome inhibition upon intravenous (IV) administration to experimental animals such as mice and rats

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Samanthula, Kumara Swamy, Agaiah Goud Bairi, and CB Mahendra Kumar. "Muco-adhesive buccal tablets of candesartan cilexetil for oral delivery: preparation, in-vitro and ex-vivo evaluation." Journal of Drug Delivery and Therapeutics 11, no. 1-s (2021): 35–42. http://dx.doi.org/10.22270/jddt.v11i1-s.4547.

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Candesartan cilexetil (CC) is an angiotensin II-receptor blocker (ARB). The antihypertensive effect of CC 4-16 mg/day was as great as that of other once-daily dosage regimens. Candesartan cilexetil has high first-pass metabolism and low oral bioavailability. The bioavailability of such drugs may be significantly improved if delivered through the buccal route; hence mucosal delivery is one of the alternative methods of systemic drug delivery. This study’s objective was to develop mucoadhesive buccal tablets of candesartan cilexetil using carbopol-934P, hydroxyl propyl methyl cellulose (HPMC), E

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Anwar, Walid, Hamdy Dawaba, Mohsen Afouna, Ahmed Samy, Mohammed Rashed, and Abdelaziz Abdelaziz. "Enhancing the Oral Bioavailability of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers: In Vitro Characterization and Absorption in Rats after Oral Administration." Pharmaceutics 12, no. 11 (2020): 1047. http://dx.doi.org/10.3390/pharmaceutics12111047.

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Candesartan Cilexetil (CC) is a prodrug widely used in the treatment of hypertension and heart failure, but it has some limitations, such as very poor aqueous solubility, high affinity to P-glycoprotein efflux mechanism, and hepatic first-pass metabolism. Therefore, it has very low oral bioavailability. In this study, glyceryl monostearate (GMS) and Capryol™ 90 were selected as solid and liquid lipids, respectively, to develop CC-NLC (nanostructured lipid carrier). CC was successfully encapsulated into NLP (CC-NLC) to enhance its oral bioavailability. CC-NLC was formulated using a hot homogeni

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Katamesh, Ahmed A., Hend Mohamed Abdel-Bar, Rania Mahafdeh, et al. "Tunable Intranasal Polymersome Nanocarriers Triggered Olanzapine Brain Delivery and Improved In Vivo Antipsychotic Activity." Pharmaceutics 17, no. 7 (2025): 811. https://doi.org/10.3390/pharmaceutics17070811.

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Background: Olanzapine (Ola) is a second-generation antipsychotic with clinical utility limited by poor brain bioavailability due to blood–brain barrier restriction, hepatic first-pass metabolism, and systemic side effects. This study aimed to develop and optimize a novel intranasal polymersome-based nanocarrier (PolyOla) to enhance brain targeting, therapeutic efficacy, and safety of Ola. Methods: PolyOla was prepared using poloxamer 401 and optimized through a Box–Behnken Design to minimize particle size and maximize entrapment (EE%) and loading efficiency (LE%). The formulation was characte

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Okada, Akie, Rina Niki, Yutaka Inoue, et al. "Development of Self-Administered Formulation to Improve the Bioavailability of Leuprorelin Acetate." Pharmaceutics 14, no. 4 (2022): 785. http://dx.doi.org/10.3390/pharmaceutics14040785.

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In recent years, the development of self-injectable formulations has attracted much attention, and the development of formulations to control pharmacokinetics, as well as drug release and migration in the skin, has become an active research area. In the present study, the development of a lipid-based depot formulation containing leuprorelin acetate (LA) as an easily metabolizable drug in the skin was prepared with a novel non-lamellar liquid-crystal-forming lipid of mono-O-(5,9,13-trimethyl-4-tetradecenyl) glycerol ester (MGE). Small-angle X-ray scattering, cryo-transmission electron microscop

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Budhwani, Karim I., Makena A. Dettmann, Mansoor N. Saleh, and Vinoy Thomas. "Nano and Microbubble Systems for On-Demand Cancer Drug Delivery." Current Nanoscience 14, no. 1 (2017): 33–41. http://dx.doi.org/10.2174/1573413713666171009160858.

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Background: Chemotherapy, the predominant cancer treatment modality, suffers from elimination in renal and hepatic systems causing reduced bioavailability and increased toxicity leading to harmful side effects. Targeted release of formulations encapsulated in protective biocompatible polymer or polymer-lipid microbubbles can improve bioavailability and potency while reducing systemic toxicity, resulting in a higher therapeutic index. Objective: Double emulsion, the most common method for microbubble fabrication suffers from low encapsulation efficiency and wide size distributions. In this conc

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Omidian, Hossein, Erma J. Gill, Sumana Dey Chowdhury, and Luigi X. Cubeddu. "Chitosan Nanoparticles for Intranasal Drug Delivery." Pharmaceutics 16, no. 6 (2024): 746. http://dx.doi.org/10.3390/pharmaceutics16060746.

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This manuscript explores the use of nanostructured chitosan for intranasal drug delivery, targeting improved therapeutic outcomes in neurodegenerative diseases, psychiatric care, pain management, vaccination, and diabetes treatment. Chitosan nanoparticles are shown to enhance brain delivery, improve bioavailability, and minimize systemic side effects by facilitating drug transport across the blood–brain barrier. Despite substantial advancements in targeted delivery and vaccine efficacy, challenges remain in scalability, regulatory approval, and transitioning from preclinical studies to clinica

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Kopecky, Jan, Martin Rossmeisl, Pavel Flachs, et al. "n-3 PUFA: bioavailability and modulation of adipose tissue function." Proceedings of the Nutrition Society 68, no. 4 (2009): 361–69. http://dx.doi.org/10.1017/s0029665109990231.

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Adipose tissue has a key role in the development of metabolic syndrome (MS), which includes obesity, type 2 diabetes, dyslipidaemia, hypertension and other disorders. Systemic insulin resistance represents a major factor contributing to the development of MS in obesity. The resistance is precipitated by impaired adipose tissue glucose and lipid metabolism, linked to a low-grade inflammation of adipose tissue and secretion of pro-inflammatory adipokines. Development of MS could be delayed by lifestyle modifications, while both dietary and pharmacological interventions are required for the succe

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