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Статті в журналах з теми "Dermatokinetics"

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Автор: Grafiati

Опубліковано: 24 січня 2023

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1

Narula, Priyanka, Komal Saini, Megha Saini, Dinesh Singla, Anurag Singh Chauhan, and Vandita Kakkar. "Assay and Dermatokinetics of Tetrahydrocurcumin Lipidic Nanostructures Using Reverse Phase-high Performance Liquid Chromatography." Pharmaceutical Nanotechnology 9, no. 2 (March 12, 2021): 130–40. http://dx.doi.org/10.2174/2211738509999210128203251.

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Background:: Envisaging the poor solubility (56 ngml1) and permeability of tetrahydrocurcumin (THCC), it was formulated into lipidic nanostructures to enhance its bioavailability upon topical application to promote the healing process for skin inflammatory disorders. Lack of literature on a suitable method for determining THCC per se and nanoformulations prompted us to develop an RP-HPLC method to detect the drug in its nanostructures and in pig ear skin post dermatokinetics. Objective:: The present investigation aimed to develop a simple, precise and RP-HPLC method for the quantitative estimation of THCC in prepared lipidic nanostructures, its ointment, and in skin homogenate obtained post dermatokinetic study. Method:: THCC encapsulated nanostructures and ointment were formulated using a modified emulsification method and embedded into an ointment base to enhance its spreadability and improve patient compliance. A fast and sensitive reverse-phase high-performance liquid chromatography method was developed using a Hypersil BDS reverse phase C18 column (4.6 mm × 250 mm, 5 μm) with mobile phase comprising tetrahydrofuran (THF) and 1 mgmL-1 citric acid (4:6), at a flow rate of 1.0 mLmin-1 with a run time of 20 min. Result:: THCC nanostructures were successfully prepared using the spontaneous microemulsification method. THCC was detected at 282 nm and revealed two peaks which were attributed to the keto-enol tautomerism in the molecule with retention times of 6.23 min and 11.06 min, respectively. The assay of THCC in nanostructures and ointment was found to be 98.30 % and 99.98 %, with an entrapment efficiency 77.00±2.74 %. The dermatokinetic studies revealed sufficient release of THCC from its ointment up to 24 hr with a concentration of 1382 μgcm-2, for causing a therapeutic effect. Conclusion:: The method was found to be reproducible and robust, as shown by the low coefficient of variation and a constant analyte/IS ratio. It was successfully employed for the estimation of THCC assay in nanostructures and its ointment and dermatokinetic analysis in the skin.

2

Nair, Anroop, Shery Jacob, Bandar Al-Dhubiab, Mahesh Attimarad, and Sree Harsha. "Basic considerations in the dermatokinetics of topical formulations." Brazilian Journal of Pharmaceutical Sciences 49, no. 3 (September 2013): 423–34. http://dx.doi.org/10.1590/s1984-82502013000300004.

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Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form. However, determining drug concentration in the skin layers following topical application of dermatological formulations is a great challenge. The protocols followed in oral formulations could not be applied for topical dosage forms. The regulatory agencies are considering several possible approaches such as tape stripping, microdialysis etc. On the other hand, the skin bioavailability assessment of xenobiotics is equally important for topical formulations in order to evaluate the toxicity. It is always possible that drug molecules applied on the skin surface may transport thorough the skin and reaches systemic circulation. Thus the real time measurement of molecules in the skin layer has become obligatory. In the last two decades, quite a few investigations have been carried out to assess the skin bioavailability and toxicity of topical/dermatological products. This review provides current understanding on the basics of dermatokinetics, drug depot formation, skin metabolism and clearance of drug molecules from the skin layers following application of topical formulations.

3

Thotakura, Nagarani, Pramod Kumar, Sheetu Wadhwa, Kaisar Raza, and Prakash Katare. "Dermatokinetics as an Important Tool to Assess the Bioavailability of Drugs by Topical Nanocarriers." Current Drug Metabolism 18, no. 5 (May 23, 2017): 404–11. http://dx.doi.org/10.2174/1389200218666170306104042.

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4

Thakur, Kanika, Gajanand Sharma, Bhupindar Singh, and Om Prakash Katare. "Topical Drug Delivery of Anti-infectives Employing Lipid-Based Nanocarriers: Dermatokinetics as an Important Tool." Current Pharmaceutical Design 24, no. 43 (March 28, 2019): 5108–28. http://dx.doi.org/10.2174/1381612825666190118155843.

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Background:The therapeutic approaches for the management of topical infections have always been a difficult approach due to lack of efficacy of conventional topical formulations, high frequency of topical applications and non-patient compliance. The major challenge in the management of topical infections lies in antibiotic resistance which leads to severe complications and hospitalizations resulting in economic burden and high mortality rates.Methods:Topical delivery employing lipid-based carriers has been a promising strategy to overcome the challenges of poor skin permeation and retention along with large doses which need to be administered systemically. The use of lipid-based delivery systems is a promising strategy for the effective topical delivery of antibiotics and overcoming drug-resistant strains in the skin. The major systems include transfersomes, niosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion and nanoemulsion as the most promising drug delivery approaches to treat infectious disorders. The main advantages of these systems include lipid bilayer structure which mimics the cell membrane and can fuse with infectious microbes. The numerous advantages associated with nanocarriers like enhanced efficacy, improvement in bioavailability, controlled drug release and ability to target the desired infectious pathogen have made these carriers successful.Conclusion:Despite the number of strides taken in the field of topical drug delivery in infectious diseases, it still requires extensive research efforts to have a better perspective of the factors that influence drug permeation along with the mechanism of action with regard to skin penetration and deposition. The final objective of the therapy is to provide a safe and effective therapeutic approach for the management of infectious diseases affecting topical sites leading to enhanced therapeutic efficacy and patient-compliance.

5

Saini, Komal, Nancy Modgill, Kamalinder Singh, and Vandita Kakkar. "Tetrahydrocurcumin Lipid Nanoparticle Based Gel Promotes Penetration into Deeper Skin Layers and Alleviates Atopic Dermatitis in 2,4-Dinitrochlorobenzene (DNCB) Mouse Model." Nanomaterials 12, no. 4 (February 14, 2022): 636. http://dx.doi.org/10.3390/nano12040636.

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Treatment of atopic dermatitis (AD) is challenging due to its complex pathophysiology. Tetrahydrocurcumin (THC) a polyphenolic, colorless compound that is more polar than curcumin. It possesses superior anti-inflammatory properties and has a clinical advantage over curcumin. The present study investigated the therapeutic effectiveness of THC solid lipid nanoparticle (THC-SLN)-based gels in AD. THC-SLNs prepared using microemulsification resulted in a particle size of 109.2 nm as determined by nanoparticle tracking, and FTIR confirmed the entrapment of drug within the lipid matrix. THC-SLNs greatly enhanced skin hydration when tested both ex vivo and in vivo in Lacca mice. Deeper skin penetration was clearly established using dermatokinetics and CLSM. The in vivo pharmacodynamics of THC-SLNs gel in 2,4-dinitrochlorobenzene (DNCB)-induced AD mice showed enhanced bioactivity; reduced levels of TNF-α and IL-6; and complete healing, as evident from histopathological studies. Thus, the novel topical THC-SLN gel has potential to emerge as a safe alternative to conventional corticosteroids for AD and other skin disorders with overbearing inflammation.

6

Leite, Marcel Nani, Juliana Santos Rosa Viegas, Fabíola Silva Garcia Praça, Natália Aparecida de Paula, Leandra Náira Zambelli Ramalho, Maria Vitória Lopes Badra Bentley, and Marco Andrey Cipriani Frade. "Ex vivo model of human skin (hOSEC) for assessing the dermatokinetics of the anti-melanoma drug Dacarbazine." European Journal of Pharmaceutical Sciences 160 (May 2021): 105769. http://dx.doi.org/10.1016/j.ejps.2021.105769.

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7

Negi, Poonam, Bhupinder Singh, Gajanand Sharma, Sarwar Beg, and Om Prakash Katare. "Biocompatible lidocaine and prilocaine loaded-nanoemulsion system for enhanced percutaneous absorption: QbD-based optimisation, dermatokinetics andin vivoevaluation." Journal of Microencapsulation 32, no. 5 (June 11, 2015): 419–31. http://dx.doi.org/10.3109/02652048.2015.1046513.

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8

Buist, Harrie E., Cees de Heer, Johan A. van Burgsteden, and Johannes J. M. van de Sandt. "Dermatokinetics of didecyldimethylammonium chloride and the influence of some commercial biocidal formulations on its dermal absorption in vitro." Regulatory Toxicology and Pharmacology 48, no. 1 (June 2007): 87–92. http://dx.doi.org/10.1016/j.yrtph.2007.01.007.

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9

Thakur, Kanika, Gajanand Sharma, Bhupinder Singh, Sanjay Chhibber, and Om Prakash Katare. "Nano-engineered lipid-polymer hybrid nanoparticles of fusidic acid: an investigative study on dermatokinetics profile and MRSA-infected burn wound model." Drug Delivery and Translational Research 9, no. 4 (January 16, 2019): 748–63. http://dx.doi.org/10.1007/s13346-019-00616-3.

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10

Iqubal, Mohammad Kashif, Ashif Iqubal, Khalid Imtiyaz, M. Moshahid A. Rizvi, Madan Mohan Gupta, Javed Ali, and Sanjula Baboota. "Combinatorial lipid-nanosystem for dermal delivery of 5-fluorouracil and resveratrol against skin cancer: Delineation of improved dermatokinetics and epidermal drug deposition enhancement analysis." European Journal of Pharmaceutics and Biopharmaceutics 163 (June 2021): 223–39. http://dx.doi.org/10.1016/j.ejpb.2021.04.007.

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11

Alam, Aftab, Mohammed H. Alqarni, Ahmed I. Foudah, Mohammad Raish, and Mohamad Ayman Salkini. "Babchi Oil-Based Nanoemulsion Hydrogel for the Management of Psoriasis: A Novel Energy Economic Approach Employing Biosurfactants." Gels 8, no. 12 (November 23, 2022): 761. http://dx.doi.org/10.3390/gels8120761.

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The current research aimed to assess the Babchi oil nanoemulsion-based hydrogel prepared using biosurfactants through a low-energy emulsification process for the topical management of psoriasis. The emulsification capacity and solubilities of many nanoemulsion constituents such as surfactants, co-surfactants, and oil were considered to determine the range of concentration of the constituents. Pseudoternary phase diagrams were created using the method of titration. Nanoemulgel structure, morphology, micromeritics, conductivity, and viscosity were all optimized. The assessment of the Babchi oil nanoemulgel included particle size, polydispersity index (PDI), drug content, pH, spreadability, rheological management, ex vivo drug study, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability, in vitro drug release, release kinetics, and dermatokinetics. The selected ratios of the surfactant mixture (Smix) taken were 3:1. The entrapment efficiency estimated was 91.298%. The zeta potential of Babchi oil was observed to be −24.93 mV at 25 °C with water as a dispersant, viscosity as 0.887 cP, and material absorption as 0.01 nm. The size distribution of the particle was 108 nm by the intensity and the conductivity observed was 0.03359 mS/cm. The cumulative amount of Babchi oil penetrated and fluxed by nanoemulgel was considered larger (p ≤ 0.05) than the conventional formulations. Skin retention was observed to be good with decreased lag time. The formulation followed the Higuchi Korsmeyer for Fickian Peppas model for in vitro drug release studies. The oil was most effective on the epidermal layer of the skin for treatment. It was established that the Babchi oil nanoemulgel formulation had superior permeability capabilities for topical and transdermal administration and is a viable alternative to traditional formulations.

12

Ali, Amena, Abuzer Ali, Mohammad Akhlaquer Rahman, Musarrat Husain Warsi, Mohammad Yusuf, and Prawez Alam. "Development of Nanogel Loaded with Lidocaine for Wound-Healing: Illustration of Improved Drug Deposition and Skin Safety Analysis." Gels 8, no. 8 (July 26, 2022): 466. http://dx.doi.org/10.3390/gels8080466.

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A wound refers to a cut or blow that may result in primary or secondary infection or even death, if untreated. In the current study, we have explored the wound-healing properties of lidocaine nanogel, owing to its antioxidant and neutrophilic modulatory potential. Initially, the pre-formulation study was performed and then using central composite design (CCD) fabrication and the characterization of lidocaine-loaded nanoemulsion was carried out. After the preparation of a nanogel of lidocaine-loaded nanoemulsion, it was evaluated on various parameters, such as pH, spreadability, extrudability, drug content, in vitro drug release, dermatokinetic study and in vivo skin safety. Based on the pre-formulation study, the maximum solubility of lidocaine was found in oleic acid (324.41 ± 4.19 mg/mL) and in Tween 20 (192.05 ± 8.25 mg/mL), selected as a suitable emulsifier. The refractive index of the optimized nanoemulsion was found to be 1.35 ± 0.04, the electrokinetic potential was recorded as −15.47 ± 0.95 mV. The pH, spreadability and extrudability of nanogel was found to be 6.87 ± 0.51, 73.32 ± 4.59 gm.cm/sec and 107.41 ± 6.42 gm/cm2, respectively. The percentage of the cumulative drug content and drug release from nanogel was found to be 99.94 ± 1.70% and 93.00 ± 4.67%, respectively. Moreover, dermatokinetic study showed significantly (p < 0.0005) improved drug deposition and the in vivo skin safety study showed no sign of dermal erythematous lesion or any visible damage. Stability studies also testified the secureness of nanogel after storage in a prescribed environmental condition. Thus, this study provides substantial evidence for healing wounds effectively and the further evaluation of the in vivo model. The patent related to this work was published in the Indian Official Journal of the Patent Office (Issue number: 20/2022).

13

Raza, Kaisar, Bhupinder Singh, Saloni Singla, Sheetu Wadhwa, Babita Garg, Sanjay Chhibber, and Om Prakash Katare. "Nanocolloidal Carriers of Isotretinoin: Antimicrobial Activity against Propionibacterium acnes and Dermatokinetic Modeling." Molecular Pharmaceutics 10, no. 5 (April 12, 2013): 1958–63. http://dx.doi.org/10.1021/mp300722f.

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14

Kumar, Neeraj, Balraj Saini, and Rajwinder Kaur. "A nontoxic ionic liquid composition for the delivery of biological macromolecular anions across the skin barrier." Pharmaceutical Patent Analyst 10, no. 4 (July 2021): 191–94. http://dx.doi.org/10.4155/ppa-2021-0012.

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The development of biocompatible ionic liquids is needed in order to explore their vastly underutilized pharmaceutical potential. US10912834 patent discloses ionic liquids comprising macromolecular biological anions and alkylated cations, which provides enhanced dermal delivery and cell internalization of the large biological anions. The studies of ex vivo permeation through excised pig skin indicated significantly higher skin penetration of percent dose and enhanced drug internalization was achieved using these ionic liquids. Although, the patent advances an infant field of biological macromolecule-based ionic liquids, the evaluation of these claimed ionic liquids relies only on the in vivo cytotoxicity data and ex vivo skin permeation behavior. Exhaustive studies, including dermatokinetic evaluation and long-term animal toxicity experiments, should be performed in order to unravel the potential of the aforementioned ionic liquids.

15

Sharma, Gajanand, Mandeep Kaur Saini, Kanika Thakur, Namarta Kapil, Neeraj Kumar Garg, Kaisar Raza, Vijay G. Goni, Anil Pareek, and Om Prakash Katare. "Aceclofenac cocrystal nanoliposomes for rheumatoid arthritis with better dermatokinetic attributes: a preclinical study." Nanomedicine 12, no. 6 (March 2017): 615–38. http://dx.doi.org/10.2217/nnm-2016-0405.

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16

Sharma, Gajanand, Geeta Dhankar, Kanika Thakur, Kaisar Raza, and O. P. Katare. "Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises." AAPS PharmSciTech 17, no. 5 (December 15, 2015): 1221–31. http://dx.doi.org/10.1208/s12249-015-0464-0.

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17

Sharma, Gajanand, Manmeet Kaur, Kaisar Raza, Kanika Thakur та O. P. Katare. "Aceclofenac–β-cyclodextrin-vesicles: a dual carrier approach for skin with enhanced stability, efficacy and dermatokinetic profile". RSC Advances 6, № 25 (2016): 20713–27. http://dx.doi.org/10.1039/c5ra24516h.

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The aim of the current investigation was to develop and characterize lipid-based carriers of aceclofenac (ACE) with enhanced stability and transdermal delivery potential to the inflammatory sites in osteoarthritis.

18

Kumar, Pramod, Rajendra Kumar, Bhupinder Singh, Ruchi Malik, Gajanand Sharma, Deepak Chitkara, O. P. Katare, and Kaisar Raza. "Biocompatible Phospholipid-Based Mixed Micelles for Tamoxifen Delivery: Promising Evidences from In - Vitro Anticancer Activity and Dermatokinetic Studies." AAPS PharmSciTech 18, no. 6 (December 13, 2016): 2037–44. http://dx.doi.org/10.1208/s12249-016-0681-1.

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19

Iqbal, Babar, Javed Ali, and Sanjula Baboota. "Silymarin loaded nanostructured lipid carrier: From design and dermatokinetic study to mechanistic analysis of epidermal drug deposition enhancement." Journal of Molecular Liquids 255 (April 2018): 513–29. http://dx.doi.org/10.1016/j.molliq.2018.01.141.

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20

Mahmood, Arisha, Vamshi Krishna Rapalli, Tejashree Waghule, Srividya Gorantla, and Gautam Singhvi. "Luliconazole loaded lyotropic liquid crystalline nanoparticles for topical delivery: QbD driven optimization, in-vitro characterization and dermatokinetic assessment." Chemistry and Physics of Lipids 234 (January 2021): 105028. http://dx.doi.org/10.1016/j.chemphyslip.2020.105028.

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21

Qadir, Abdul, Mohd Aqil, Athar Ali, Musarrat Husain Warsi, Mohd Mujeeb, Farhan J. Ahmad, Sayeed Ahmad, and Sarwar Beg. "Nanostructured lipidic carriers for dual drug delivery in the management of psoriasis: Systematic optimization, dermatokinetic and preclinical evaluation." Journal of Drug Delivery Science and Technology 57 (June 2020): 101775. http://dx.doi.org/10.1016/j.jddst.2020.101775.

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22

Permana, McCrudden, and Donnelly. "Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study." Pharmaceutics 11, no. 7 (July 17, 2019): 346. http://dx.doi.org/10.3390/pharmaceutics11070346.

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Conventional oral administration of antifilariasis drugs results in nonspecific targeting of the drugs and the intradermal delivery of nanoparticles with sizes of <100 nm could be used to improve lymphatic uptake. This study investigated the combination of nanosuspension and dissolving microneedles (MN-NS) as an alternative intradermal delivery approach for the delivery of antifilariasis drugs, namely doxycycline, albendazole, and ivermectin. NS were fabricated and optimized using a bottom-up technique. The NS were then incorporated into the MN arrays. The optimized NS were <100 nm in diameter. Furthermore, MN-NS had suitable mechanical strength and insertion capabilities. The dermatokinetic study revealed that the delivery of drugs into the dermis of excised neonatal porcine skin by MNs was significantly higher than that from a needle-free patch, with 29.29 ± 4.65%, 31.54 ± 5.35%, and 34.54 ± 4.98% of doxycycline, albendazole sulfoxide, and ivermectin retained in the dermis after 24 h. The results presented here serve as proof of concept for the significant enhancement of drug retention times in the dermis, following their formulation into NS and delivery via MN. Leading on from these studies, future work must investigate in vivo lymphatic pharmacokinetic profiling of drugs formulated into NS, in a suitable animal model.

23

Mir, Maria, Naveed Ahmed, Andi Dian Permana, Aoife Maria Rodgers, Ryan F. Donnelly, and Asim ur Rehman. "Enhancement in Site-Specific Delivery of Carvacrol against Methicillin Resistant Staphylococcus aureus Induced Skin Infections Using Enzyme Responsive Nanoparticles: A Proof of Concept Study." Pharmaceutics 11, no. 11 (November 13, 2019): 606. http://dx.doi.org/10.3390/pharmaceutics11110606.

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Methicillin resistant Staphylococcus aureus (MRSA) induced skin infections have become a challenging problem due to the escalating antibiotic resistance. Carvacrol (CAR) has been reported to be effective against MRSA. However, due to its characteristics, CAR exhibits low skin retention. In this study, CAR was formulated into site-specific nanoparticle (NPs) delivery system using poly(ε-caprolactone) (PCL), following incorporation into a hydrogel matrix to facilitate dermal delivery. The release study exhibited significantly higher release of CAR from PCL NPs in the presence of bacterial lipase, highlighting its potential for differential delivery. Moreover, encapsulation of CAR in PCL NPs resulted in a two-fold increase in its anti-MRSA activity. Dermatokinetic studies revealed that the NPs loaded hydrogel was able to enhance skin retention of CAR after 24 h (83.29 ± 3.15%), compared to free CAR-loaded hydrogel (0.85 ± 0.14%). Importantly, this novel approach exhibited effective antimicrobial activity in an ex-vivo skin infection model. Hence, these findings have proven the concept that the loading of CAR into a responsive NPs system can lead to sustained antimicrobial effect at the desired site, and may provide a novel effective approach for treatment of MRSA induced skin infections. However, further studies must be conducted to investigate in-vivo efficacy of the developed system in an appropriate infection model.

24

Chen, Lihua, Majed Alrobaian, Obaid Afzal, Imran Kazmi, Sunil K. Panda, Abdulmalik Saleh Alfawaz Altamimi, Fahad A. Al-Abbasi, et al. "Crotamiton-loaded tea tree oil containing phospholipid-based microemulsion hydrogel for scabies treatment: in vitro, in vivo evaluation, and dermatokinetic studies." Drug Delivery 28, no. 1 (January 1, 2021): 1972–81. http://dx.doi.org/10.1080/10717544.2021.1979131.

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25

Sharma, Gajanand, Shelly Kamboj, Kanika Thakur, Poonam Negi, Kaisar Raza, and O. P. Katare. "Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia." AAPS PharmSciTech 18, no. 3 (June 17, 2016): 790–802. http://dx.doi.org/10.1208/s12249-016-0561-8.

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26

Sharma, Gajanand, Neelam Devi, Kanika Thakur, Ashay Jain, and OP Katare. "Lanolin-based organogel of salicylic acid: evidences of better dermatokinetic profile in imiquimod-induced keratolytic therapy in BALB/c mice model." Drug Delivery and Translational Research 8, no. 2 (February 21, 2017): 398–413. http://dx.doi.org/10.1007/s13346-017-0364-9.

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27

Moolakkadath, Thasleem, Mohd Aqil, Abdul Ahad, Syed Sarim Imam, Babar Iqbal, Yasmin Sultana, Mohd Mujeeb, and Zeenat Iqbal. "Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies." Artificial Cells, Nanomedicine, and Biotechnology 46, sup2 (May 7, 2018): 755–65. http://dx.doi.org/10.1080/21691401.2018.1469025.

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28

Garg, Neeraj K., Gajanand Sharma, Bhupinder Singh, Pradip Nirbhavane, Rajeev K. Tyagi, Rahul Shukla, and O. P. Katare. "Quality by Design (QbD)-enabled development of aceclofenac loaded-nano structured lipid carriers (NLCs): An improved dermatokinetic profile for inflammatory disorder(s)." International Journal of Pharmaceutics 517, no. 1-2 (January 2017): 413–31. http://dx.doi.org/10.1016/j.ijpharm.2016.12.010.

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29

Rapalli, Vamshi Krishna, Swati Sharma, Aniruddha Roy, and Gautam Singhvi. "Design and dermatokinetic evaluation of Apremilast loaded nanostructured lipid carriers embedded gel for topical delivery: A potential approach for improved permeation and prolong skin deposition." Colloids and Surfaces B: Biointerfaces 206 (October 2021): 111945. http://dx.doi.org/10.1016/j.colsurfb.2021.111945.

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30

Thakur, Kanika, Akanksha Mahajan, Gajanand Sharma, Bhupinder Singh, Kaisar Raza, Sanjay Chhibber, and Om Prakash Katare. "Implementation of Quality by Design (QbD) approach in development of silver sulphadiazine loaded egg oil organogel: An improved dermatokinetic profile and therapeutic efficacy in burn wounds." International Journal of Pharmaceutics 576 (February 2020): 118977. http://dx.doi.org/10.1016/j.ijpharm.2019.118977.

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31

Mudjahid, Mukarram, Sulistiawati, Rangga Meidianto Asri, Firzan Nainu, and Andi Dian Permana. "Validation of spectrophotometric method to quantify chloramphenicol in fluid and rat skin tissue mimicking infection environment: Application to in vitro release and ex vivo dermatokinetic studies from dissolving microneedle loaded microparticle sensitive bacteria." Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 291 (April 2023): 122374. http://dx.doi.org/10.1016/j.saa.2023.122374.

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Quantin, Paul, Mathilde Stricher, Sophie Catoire, Hervé Ficheux, and Christophe Egles. "Dermatokinetics: Advances and Experimental Models, Focus on Skin Metabolism." Current Drug Metabolism 23 (May 17, 2022). http://dx.doi.org/10.2174/1389200223666220517114004.

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Abstract: Numerous dermal contact products, such as drugs or cosmetics, are applied on the skin, the first protective barrier to their entrance into the organism. These products contain various xenobiotic molecules that can penetrate the viable epidermis. Many studies have shown that keratinocyte metabolism could affect their behavior by biotransformation. While aiming for detoxification, toxic metabolites can be produced. These metabolites may react with biological macromolecules often leading to sensitization reactions. After passing through the epidermis, xenobiotics can reach the vascularized dermis and therefore be bioavailable and distributed into the entire organism. To highlight these mechanisms, dermatokinetics, based on the concept of pharmacokinetics, has been developed recently. It provides information on the action of xenobiotics that penetrate the organism through the dermal route. The purpose of this review is first to describe and synthesize the dermatokinetics mechanisms to consider when assessing the absorption of a xenobiotic through the skin. We focus on skin absorption and specifically on skin metabolism, the two main processes involved in dermatokinetics. In addition, experimental models and methods to assess dermatokinetics are described and discussed to select the most relevant method when evaluating, in a specific context, dermatokinetics parameters of a xenobiotic. We also discuss the limits of this approach as it is notably used for risk assessment in the industry where scenario studies generally focus only on one xenobiotic and do not consider interactions with the rest of the exposome. The hypothesis of adverse effects due to the combination of chemical substances in contact with individuals and not to a single molecule are being increasingly studied and embraced in the scientific community.

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Ramzan, Mohhammad, Samuel Gourion-Arsiquaud, Afzal Hussain, Jaspreet Singh Gulati, Qihong Zhang, Sonia Trehan, Vinam Puri, Bozena Michniak-Kohn, and Indu Pal Kaur. "In vitro release, ex vivo penetration, and in vivo dermatokinetics of ketoconazole-loaded solid lipid nanoparticles for topical delivery." Drug Delivery and Translational Research, January 7, 2022. http://dx.doi.org/10.1007/s13346-021-01058-6.

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34

Rahman, Mahfoozur, Obaid Afzal, Sunil K. Panda, Imran Kazmi, Ahmed Mahmoud Abdelhaleem Ali, Manal A. Alossaimi, Fahad A. Al-Abbasi, et al. "UPLC–MS/MS Method Validation for Estimation of Resveratrol in Rat Skin from Liposphere Gel Formulation and Its Application to Dermatokinetic Studies in Rats." Journal of Chromatographic Science, September 11, 2021. http://dx.doi.org/10.1093/chromsci/bmab105.

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Abstract For the quantification of resveratrol (RV) in the Wistar rat skin, an ultra-performance liquid chromatography-mass spectrometric (UPLC–MS/MS) method was developed and validated on ACQUITY UPLC BEH C18 column (1.7 μm). The mobile phase ratio of methanol (A) and 2% formic acid (B) (ratio 10: 90% v/v, 80: 20 v/v) at isocratic elution with flow rate 0.3 mL/min, and run time 3 min was used for analysis. In addition, the use of multiple reaction monitoring (MRM)/ES+ mode to detect the analytes and to track parents to daughter ion transition of 229.17 > 107.04 m/z (time scan 3 min, retention time 1.48) for RV and curcumin as an internal standard shows 369.16 > 176.93m/z (scan time is 2.80 min, retention time is 1.11), respectively. Linearity was observed in the range of 2.5 to 2,000 ng/mL (R2 = 0.987). Precision and accuracy on rat skin were within the acceptability range (RE%: ±15; RSD%: ±15). Moreover, it showed a good percentage recovery and found within acceptance limit 90–110%. Lower limit of detection and quantitation for the method observed to be 2.5 and 20 ng.mL−1, respectively. Method application indicated successful determination of dermatokinetics parameters of RV from lipospheres gel and suspension in the rats.

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Gorantla, Srividya, Ranendra N. Saha, and Gautam Singhvi. "Design of experiment-driven stability-indicating RP-HPLC method for the determination of tofacitinib in nanoparticles and skin matrix." Future Journal of Pharmaceutical Sciences 7, no. 1 (August 30, 2021). http://dx.doi.org/10.1186/s43094-021-00325-0.

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Abstract Background Tofacitinib—an oral JAK inhibitor—has been recently approved by US FDA to treat moderate to severe RA. The delivery of tofacitinib to specific inflammation site at joint via topical route using nanoformulations helps in managing the potential adverse effects. The objective is to develop and validate a simple, specific, and sensitive stability-indicating HPLC method for quantification of tofacitinib in topical nanoformulations and different matrices (adhesive tape, and skin layers, i.e., stratum corneum, viable epidermis, and dermis). The major objective was to avoid use of instruments like LC–MS/MS and to ensure a widespread application of the method. Result A 32 factorial ‘design of experiments’ was applied to optimize process variables, to understand the effect of variables on peak properties. The calibration curve showed regression coefficient (R2) 0.9999 and linearity in the concentration range of 50 to 15,000 ng/mL, which is suitable for the analysis of conventional dosage forms and nanoformulations. Method validation was performed as per ICH guideline Q2 (R1). The accuracy by recovery studies ranged between 98.09 and 100.82%. The % relative standard deviations in intraday and interday precisions were in the range of 1.16–1.72 and 1.22–1.80%, respectively. Forced degradation studies indicated the specificity of method and showed stability-indicating potential for tofacitinib peak. Conclusion The validated method provides a quantification method of tofacitinib in the presence of formulation excipients, dissolution media, and skin tissues in detail. In addition, the method was successfully utilized for determination of various dermatokinetics profile of tofacitinib.

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Alqahtani, Safar M., Ali Altharawi, Majed Alrobaian, Waleed H. Almalki, Alhumaidi B. Alabbas, Shehla Nasar Mir Najib Ullah, Tanuja Singh, et al. "UPLC–MS/MS Method Development for Simultaneous Estimation of Diclofenac and Resveratrol-Loaded Liposomal Gel Formulation in Mice Skin Model: Application to Dermatokinetic Study." Journal of Chromatographic Science, January 14, 2023. http://dx.doi.org/10.1093/chromsci/bmac109.

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Abstract The current research work describes the development of a simple, fast, sensitive and efficient bioanalytical UPLC/MS–MS method for the simultaneous estimation of diclofenac and resveratrol in mice skin samples. Quetiapine was used as an internal standard (IS). Analytical separation was performed on ACQUITY UPLC C18 Column (2.1 × 100 mm; 1.7 μm) using ammonium acetate (5 mM) in water and methanol (B) with isocratic elution at ratio of (50, 50 v/v) and flow rate of 0.4 mL/min. The duration of separation was maintained for 3 min. Electrospray ionization mass spectrometry in a positive and negative ionization mode was used for detection. Selective ion mode monitoring was used for the quantification of m/z 296.025> 249.93 for diclofenac, m/z 229.09 > 143.03 for resveratrol and MRM/ES+ve mode applied in m/z 384.25> 253.189 for IS transitions from parent to daughter ion. The lower detection and quantification limits were accomplished, and precision (repeatability and intermediate precision) with a coefficient of variation below 10% produced satisfactory results. The developed bioanalytical method was found to be useful for its suitability for the dermatokinetic evaluation of treatments through rat skin. Improvement in AUC (1.58-fold for diclofenac and 1.60-fold for resveratrol) and t1/2 in the dermis (2.13 for diclofenac and 2.21-fold for resveratrol) followed by epidermis was observed for diclofenac and resveratrol-loaded liposomal gel formulation over the conventional gel. Overall, the developed method for the dermatokinetic studies of the above-mentioned dual drugs-loaded liposome gel was found to be reproducible and effective for bioanalytical.

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Alhakamy, Nabil A., Hibah M. Aldawsari, Javed Ali, Dipak K. Gupta, Musarrat H. Warsi, Anwar L. Bilgrami, Hani Z. Asfour, Ahmad O. Noor, and Shadab Md. "Brucine-loaded transliposomes nanogel for topical delivery in skin cancer: statistical optimization, in vitro and dermatokinetic evaluation." 3 Biotech 11, no. 6 (May 22, 2021). http://dx.doi.org/10.1007/s13205-021-02841-5.

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Ahmad, Niyaz, Mohammed Saifuddin Khalid, Mohd Faiyaz Khan, and Zabih Ullah. "Beneficial effects of topical 6-gingerol loaded nanoemulsion gel for wound and inflammation management with their comparative dermatokinetic." Journal of Drug Delivery Science and Technology, December 2022, 104094. http://dx.doi.org/10.1016/j.jddst.2022.104094.

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Krumpholz, Laura, James F. Clarke, Sebastian Polak, and Barbara Wiśniowska. "An open-access data set of pig skin anatomy and physiology for modelling purposes." Database 2022 (January 1, 2022). http://dx.doi.org/10.1093/database/baac091.

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Abstract The use of animal as opposed to human skin for in vitro permeation testing (IVPT) is an alternative, which can reduce logistical and economic issues. However, this surrogate also has ethical considerations and may not provide an accurate estimation of dermal absorption in humans due to physiological differences. The current project aimed to provide a detailed repository for the anatomical and physiological parameters of porcine skin, with the aim of parametrizing the Multi-phase Multi-layer Mechanistic Dermal Absorption (MPML MechDermA) Model in the Simcyp Simulator. The MPML MechDermA Model is a physiologically based pharmacokinetic (PBPK) model that accounts for the physiology and geometry of skin in a mechanistic mathematical modelling framework. The database provided herein contains information on 14 parameters related to porcine skin anatomy and physiology, namely, skin surface pH, number of stratum corneum (SC) layers, SC thickness, corneocyte thickness, corneocyte dimensions (length and width), volume fraction of water in corneocyte (where SC is divided into four parts with different water contents), intercellular lipid thickness, viable epidermis thickness, dermis thickness, hair follicle and hair shaft diameter, hair follicle depth and hair follicle density. The collected parameters can be used to parameterize PBPK models, which could be further utilized to bridge the gap between animal and human studies with interspecies extrapolation or to predict dermatokinetic properties typically assessed in IVPT experiments. Database URL: https://data.mendeley.com/datasets/mwz9xv4cpd/1

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Garg, Neeraj K., Nikunj Tandel, Sanjay Kumar Bhadada, and Rajeev K. Tyagi. "Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases." Frontiers in Pharmacology 12 (September 20, 2021). http://dx.doi.org/10.3389/fphar.2021.713616.

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Aceclofenac (ACE), a cyclooxygenase-2 inhibitor, is the derivative of the diclofenac group that has been in use for the symptomatic treatment of systemic inflammatory autoimmune disease, rheumatoid arthritis (RA). Partial solubility, high lipophilic nature, and stability challenge its use in developing topical formulations. Hence, we developed and characterized nanostructured lipid carrier (NLC)–based ACE (ACE-NLC) hydrogel for an efficient transdermal delivery. NLC microemulsion was prepared using different lipids by various methods and was characterized with respect to particle size, zeta potential, surface morphology, and drug encapsulation efficiency. The optimized NLC formulation was incorporated into Carbopol® 940 gel, and this arrangement was characterized and compared with the existing marketed gel (Mkt-gel) formulation to assess in vitro drug release, rheology, texture profile, in vivo skin retention and permeation, and stability. Furthermore, prepared and characterized ACE-loaded NLC formulation was evaluated for skin integrity and fitted in a dermatokinetic model. The results of this study confirmed the spherical shape; smooth morphology and nanometric size attested by Zetasizer and scanning and transmission electron microcopy; and stability of the ACE-NLC formulation. The ACE-NLC-gel formulation showed good rheological and texture characteristics, and better skin distribution in the epidermis and dermis. Moreover, ACE-NLC permeated deeper in the skin layers and kept the skin integrity intact. Overall, NLC-based gel formulation of ACE might be a promising nanoscale lipid carrier for topical application when compared with the conventional Mkt-gel formulation.

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Sharma, Mandeep, Gajanand Sharma, Bhupinder Singh, and Om Prakash Katare. "Systematically Optimized Imiquimod-Loaded Novel Hybrid Vesicles by Employing Design of Experiment (DoE) Approach with Improved Biocompatibility, Stability, and Dermatokinetic Profile." AAPS PharmSciTech 20, no. 4 (March 29, 2019). http://dx.doi.org/10.1208/s12249-019-1331-1.

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Bhargav, Eranti, Yiragamreddy Padmanabha Reddy, and Koteshwara Kunnatur B. "Development and optimization of Luliconazole Nanostructured lipid carriers based gel by Quality by Design its skin distribution studies, dermatokinetic modeling & In-vitro and Ex-vivo correlation." Current Drug Delivery 18 (December 14, 2020). http://dx.doi.org/10.2174/1567201818666201214145818.

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Objective : The present study was aimed to improve the permeability of Luliconazole (LZ) and to localize high drug concentrations at skin layers by Quality by Design (QbD) based Nanostructured lipid carriers (NC) based gel. Methods: Quality Target Product Profile was set and Critical Quality attributes were identified. FT-IR and DSC studies confirmed compatibility. Risk assessment was carried out by screening the factors using 27-27-2 fractional factorial design and optimization by Box Behnken design. Cholesterol: Cetyl Palmitate, PEG 200 and probe sonication time were identified as factors, Particle size (<200 nm), PDI (0.4), % Entrapment efficiency (% EE, >80%) and % Cumulative Drug release (% CDR, >95%) as responses. Contour plots, Overlay plots and desirability were utilized to create design space. Results: The quadratic polynomial equations showed that increased lipid content, PEG 200 and optimum sonication time reduced Particle size, PDI, improved % EE and % CDR. The optimized formula was formulated into a gel. Ex-vivo permeation studies performed using pig ear pinna skin revealed that developed LZ NC gel exhibited greater permeation 272.98±8.57 (µg/cm2 ) and 32.11 ±4.7 (µg/cm2 /h) flux than plain drug dispersed gel. Dermatokinetic parameters of LZ NC gel revealed that highly significant amount of LZ was permeated, distributed and transported through the skin layers. The better linear correlations were obtained by LZ permeation through synthetic membrane (in-vitro) and pig ear pinna skin (ex-vivo). Conclusion: The above findings revealed that developed LZ NC gel exhibited better permeation and localization at skin layers in treating fungal infections.

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Raut, Prabhu, Shobhit Kumar, Babar Iqbal, Javed Ali, and Sanjula Baboota. "Development of nanoemulsion gel based formulation of terbinafine for the synergistic antifungal activity: Dermatokinetic experiment for investigation of epidermal terbinafine deposition enhancement." Inorganic and Nano-Metal Chemistry, December 20, 2020, 1–16. http://dx.doi.org/10.1080/24701556.2020.1862209.

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Mahmood, Arisha, Vamshi Krishna Rapalli, Srividya Gorantla, Tejashree Waghule, and Gautam Singhvi. "Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery: QbD-driven design, optimization, and in vitro and ex vivo evaluations." Drug Delivery and Translational Research, April 24, 2021. http://dx.doi.org/10.1007/s13346-021-00986-7.

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Asfour, Hani Z., Nabil A. Alhakamy, Md Shoaib Alam, Mohammed W. Al-Rabia, and Shadab Md. "Design of Experiment Navigated Methodical Development of Neem Oil Nanoemulsion Containing Tea Tree Oil for Dual Effect Against Dermal Illness: Ex Vivo Dermatokinetic and In Vivo." Journal of Cluster Science, July 4, 2022. http://dx.doi.org/10.1007/s10876-022-02301-x.

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