Academic literature on the topic 'Capryol 90'

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Journal articles on the topic "Capryol 90"

1

Ukai, Hiroki, Kazuki Iwasa, Takamasa Deguchi, Masaki Morishita, Hidemasa Katsumi, and Akira Yamamoto. "Enhanced Intestinal Absorption of Insulin by Capryol 90, a Novel Absorption Enhancer in Rats: Implications in Oral Insulin Delivery." Pharmaceutics 12, no. 5 (2020): 462. http://dx.doi.org/10.3390/pharmaceutics12050462.

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Labrasol® is a self-emulsifying excipient that contains saturated polyglycolysed C6–C14 glycerides and this additive is known to improve the intestinal absorption of poorly absorbed drugs after oral administration. However, the effects of formulations similar to Labrasol® on the intestinal absorption of poorly absorbed drugs have not been characterized. In this study, we used insulin as a model peptide drug and examined the absorption-enhancing effects of Labrasol® and its related formulations for insulin absorption in rats. The co-administration of Labrasol-related formulations with insulin reduced the blood glucose levels. Among these formulations, Capryol 90 was the most effective additive. Notably, the effect of Capryol 90 was greater at pH 3.0 than at pH 7.0. Additionally, almost no mucosal damage was observed in the presence of these formulations, as these formulations did not affect the activity of lactate dehydrogenase (LDH) and the amount of protein released from the small intestine. In mechanistic studies, Capryol 90 improved the stability of insulin and suppressed the association with insulin under acidic conditions. The loosening of the tight junctions (TJs) could be the underlying mechanism by which Capryol 90 improved intestinal insulin absorption via a paracellular route. These findings suggest that Capryol 90 is an effective absorption enhancer for improving the intestinal absorption of insulin, without inducing serious damage to the intestinal epithelium.
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2

Rao, Monica R. P., Shital Aghav, Girish Sukre, and Manmeet Kumar. "Determination of Required HLB of Capryol 90." Journal of Dispersion Science and Technology 35, no. 2 (2014): 161–67. http://dx.doi.org/10.1080/01932691.2013.777824.

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3

Baral, Kshitis Chandra, Jae-Geun Song, Sang Hoon Lee, et al. "Enhanced Bioavailability of AC1497, a Novel Anticancer Drug Candidate, via a Self-Nanoemulsifying Drug Delivery System." Pharmaceutics 13, no. 8 (2021): 1142. http://dx.doi.org/10.3390/pharmaceutics13081142.

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AC1497 is an effective dual inhibitor of malate dehydrogenase 1 and 2 targeting cancer metabolism. However, its poor aqueous solubility results in low bioavailability, limiting its clinical development. This study was conducted to develop an effective self-nanoemulsifying drug delivery system (SNEDDS) of AC1497 to improve its oral absorption. Based on the solubility of AC1497 in various oils, surfactants, and cosurfactants, Capryol 90, Kolliphor RH40, and Transcutol HP were selected as the components of SNEDDS. After testing various weight ratios of Capryol 90 (20–30%), Kolliphor RH40 (35–70%), and Transcutol HP (10–35%), SNEDDS-F4 containing 20% Capryol 90, 45% Kolliphor RH40, and 35% Transcutol HP was identified as an optimal SNEDDS with a narrow size distribution (17.8 ± 0.36 nm) and high encapsulation efficiency (93.6 ± 2.28%). Drug release from SNEDDS-F4 was rapid, with approximately 80% of AC1497 release in 10 min while the dissolution of the drug powder was minimal (<2%). Furthermore, SNEDDS-F4 significantly improved the oral absorption of AC1497 in rats. The maximum plasma concentration and area under the plasma concentration–time curve of AC1497 were, respectively 6.82- and 3.14-fold higher for SNEDDS-F4 than for the drug powder. In conclusion, SNEDDS-F4 with Capryol 90, Kolliphor RH40, and Transcutol HP (20:45:35, w/w) effectively improves the solubility and oral absorption of AC1497.
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4

Shakeel, Faiyaz, Nazrul Haq, Fars K. Alanazi, and Ibrahim A. Alsarra. "Impact of various nonionic surfactants on self-nanoemulsification efficiency of two grades of Capryol (Capryol-90 and Capryol-PGMC)." Journal of Molecular Liquids 182 (June 2013): 57–63. http://dx.doi.org/10.1016/j.molliq.2013.03.011.

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Chrastina, Adrian, John Welsh, Per Borgström, and Veronique T. Baron. "Propylene Glycol Caprylate-Based Nanoemulsion Formulation of Plumbagin: Development and Characterization of Anticancer Activity." BioMed Research International 2022 (January 10, 2022): 1–9. http://dx.doi.org/10.1155/2022/3549061.

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Plumbagin, a bioactive naphthoquinone, has demonstrated potent antitumor potential. However, plumbagin is a sparingly water-soluble compound; therefore, clinical translation requires and will be facilitated by the development of a new pharmaceutical formulation. We have generated an oil-in-water nanoemulsion formulation of plumbagin using a low-energy spontaneous emulsification process with propylene glycol caprylate (Capryol 90) as an oil phase and Labrasol/Kolliphor RH40 as surfactant and cosurfactant excipients. Formulation studies using Capryol 90/Labrasol/Kolliphor RH40 components, based on pseudoternary diagram and analysis of particle size distribution and polydispersity determined by dynamic light scattering (DLS), identified an optimized composition of excipients for nanoparticle formulation. The nanoemulsion loaded with plumbagin as an active pharmaceutical ingredient had an average hydrodynamic diameter of 30.9 nm with narrow polydispersity. The nanoemulsion exhibited long-term stability, as well as good retention of particle size in simulated physiological environments. Furthermore, plumbagin-loaded nanoemulsion showed an augmented cytotoxicity against prostate cancer cells PTEN-P2 in comparison to free drug. In conclusion, we generated a formulation of plumbagin with high loading drug capacity, robust stability, and scalable production. Novel Capryol 90-based nanoemulsion formulation of plumbagin demonstrated antiproliferative activity against prostate cancer cells, warranting thus further pharmaceutical development.
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6

Lee, Jong-Hwa, and Gye-Won Lee. "Formulation Approaches for Improving the Dissolution Behavior and Bioavailability of Tolvaptan Using SMEDDS." Pharmaceutics 14, no. 2 (2022): 415. http://dx.doi.org/10.3390/pharmaceutics14020415.

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Tolvaptan, a selective vasopressin receptor antagonist, is a Class IV agent of Biopharmaceutical Classification System (BCS). To improve bioavailability after oral administration, the new tolvaptan-loaded self-microemulsifying drug delivery system (SMEDDS) was further optimized using a “design of the experiment (DoE)” including components of D-optional mixture design. Based on a solubility study of tolvaptan in various oils, surfactants, and cosurfactants, Capryol® 90, Tween 20, and Transcutol® HP [or polyethylene glycol 200 (PEG 200)] were finally selected for optimization of tolvaptan-loaded SMEDDS formulations. The fitting models of, and poly-nominal equations for, all response variables were acceptable, as revealed by analysis of variance (ANOVA, R2 > 0.900, p < 0.0001). The optimized formulations A-1 (Capryol® 90/Tween 20/Transcutol® HP = 10%/70%/20% w/w) and B-1 (Capryol® 90/Tween 20/PEG 200 = 10%/70%/20% w/w) with desirabilities of 0.905 and 1.000, respectively, showed low droplet size and the dissolution rate exceeded 95% at 15 and 60 min. The tolvaptan-loaded SMEDDS remained stable for 3 months under accelerated conditions, thus with no change in any of content, color, particle size, or dissolution rate. In a rat pharmacokinetic study, the bioavailability of formulations A-1 (16.6%) and B-1 (11.5%) were 23–33-fold higher than that of raw tolvaptan powder (0.5%). Thus, the use of “quality by design (QbD)” during development of tolvaptan-loaded SMEDDS improved the dissolution rate and oral drug bioavailability.
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7

Mardiyanto, Mardiyanto, Najma Annuria Fithri, and Martina Tandry. "Characterization and Optimization of Capryol-90, Polysorbate-80, And Peg-400 Proportion in Mefenamic Acid Self Nanoemulsifying Drug Delivery System (SNEDDS) With Simplex-Lattice-Design." Science and Technology Indonesia 3, no. 4 (2018): 164. http://dx.doi.org/10.26554/sti.2018.3.4.164-172.

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Mefenamic acid as pain relief drug belongs to the biopharmaceutics classification system (BCS) class II which is practically insoluble in water causing extremely low dissolution in gastrointestinal tract. The self nanoemulsifying drug delivery system (SNEDDS) is a new innovation pharmaceutical dosage form that has effectively known to increase solubilization of hydrophobic drug in polar solvent. In this study the capryol-90 was selected as oil phase in SNEDDS as it showed maximal solubility of mefenamic acid (20 mg/mL). Combination of polysorbate-80 and PEG-400 as a generally regarded as safe (GRAS) excipient were used as surfactant and co-surfactant in SNEDDS due to its high HLB property that can increase mefenamic acid solubility in water. The ternary phase diagram of capryol-90, polysorbate-80, and PEG-400 was constructed in advance to obtain the component concentration of spontaneous nanoemulsion region. Model simplex-lattice-design cooperated in Design-Expert®10 was used to define SNEDDS mefenamic acid formula. Optimized mefenamic acid SNEDDS formula consisted of 20% capryol-90, 31.62% polysorbate-80, and 48.38% PEG-400. Characterization study of Optimized mefenamic acid SNEDDS formula showed improvement of drug content (102.820 ± 4.950)%, emulsification time (421.015 ± 1.290) second, and viscosity (0.927 ± 0.017) mm2/s 30oC. One way ANOVA statistical analysis result of optimal formula SNEDDS (105.210 ± 4.425)% of drug content, commercial generic caplet (0.917 ± 0.094)%, and mefenamic acid powder capsule (10.446 ± 0,333)% gave significant value (sig*) below than 0.05. Optimal formula proved that SNEDDS can significantly increase mefenamic acid dissolution of pH 7.4 (ileum fluid). The optimal formula of mefenamic acid SNEDDS successfully formed an uniformity droplet size (PDI 0.18) with mean size 241.9 nm and the surface charge has a value of -16.5 mV respectively.
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8

Kim, Han-Sol, Chang-Min Kim, An-Na Jo, and Joo-Eun Kim. "Studies on Preformulation and Formulation of JIN-001 Liquisolid Tablet with Enhanced Solubility." Pharmaceuticals 15, no. 4 (2022): 412. http://dx.doi.org/10.3390/ph15040412.

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This study aimed to develop a heat shock protein 90 (Hsp90) inhibitor liquisolid tablet with improved solubility to overcome low bioavailability issues. As an active pharmaceutical ingredient (API), JIN-001, a novel Hsp90 inhibitor, was reported to have substantial in vitro antiproliferative and in vivo antitumor activity; however, JIN-001 was a crystalline solid with very low solubility in an aqueous solution, and therefore, Capryol 90, which has excellent solubilization ability, was selected as an optimal liquid vehicle based on solubility studies. JIN-001 liquisolid (JLS) powder was successfully prepared by dissolving JIN-001 in Capryol 90 and mixing colloidal silicon dioxide (CSD) used as an oil adsorption agent. The prepared JLS was confirmed to be amorphous. Based on the result of the solubility test of JLS, compared to JIN-001, the solubility of the former was significantly improved in all solvents regardless of pH. JLS tablets were prepared through wet granulation using JIN-001 and stable excipients based on the compatibility test. The developed JLS tablet significantly increased the drug release rate in all tested solutions; however, the liquisolid method had no significant effect on bioavailability in the pharmacokinetics study in beagle dogs. In conclusion, the liquisolid system influenced the solubility and dissolution rate of JIN-001.
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9

Wijayanti, Ifa Rizki, Ilham Kuncahyo, and Wiwin Herdwiani. "Skrining dan Karakterisasi Komponen Self Nano Emulsifying Drug Delivery System (SNEDDS) Atorvastatin Menggunakan Fractional Factorial Design (FFD)." Jurnal Mandala Pharmacon Indonesia 10, no. 2 (2024): 346–55. https://doi.org/10.35311/jmpi.v10i2.546.

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Atorvastatin merupakan obat yang memiliki kelarutan rendah dalam air (BCS kelas II) serta memiliki aktivitas farmakologis sebagai terapi hiperkolesterolemia. Self?nanoemulsifying drug delivery systems (SNEDDS) dianggap sebagai pendekatan yang potensial untuk meningkatkan kelarutan atorvastatin karena stabil dan proses pembuatan yang relatif sederhana. Penelitian ini bertujuan untuk memilih komponen dan rasio komponen SNEDDS atorvastatin menggunakan pendekatan desain faktorial terfraksi (DFT) terhadap parameter waktu emulsifikasi, ukuran droplet, indeks polidispersitas (PDI), zeta potensial, persen transmitan, dan loading obat. Variabel yang digunakan dalam pengembangan SNEDDS atorvastatin adalah tipe dan konsentrasi minyak (capryol 90 dan asam oleat), surfaktan (cremophor RH40 dan tween 80), dan ko-surfaktan (transcutol dan PEG 400). Hasil DFT didapatkan 16 run dengan perbedaan proporsi komponen SNEDDS atorvastatin, kemudian dilakukan karakterisasi parameter kritis meliputi waktu emulsifikasi, persen transmitan, ukuran droplet, loading obat, indeks polidispersitas, dan zeta potensial. Komponen dan rasio komponen SNEDDS atorvastatin ditentukan dengan analisa single factor plot menggunakan program design expert 13. Hasil penelitian menunjukkan capryol 90, cremophor RH40, dan transcutol terpilih sebagai komponen minyak, surfaktan, dan ko?surfaktan yang memiliki kontribusi paling besar dalam pembuatan SNEDDS atorvastatin dengan rasio minyak pada 11,1-37,5 %, rasio surfaktan 36,4-77,8 %, rasio ko-surfaktan 11,1-44,4 %.
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10

Ansari, Muhammad Mohsin, Dang-Khoa Vo, Ho-Ik Choi, et al. "Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability." Pharmaceutics 15, no. 8 (2023): 2073. http://dx.doi.org/10.3390/pharmaceutics15082073.

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Poor aqueous solubility and dissolution limit the oral bioavailability of Biopharmaceutics Classification System (BCS) class II drugs. In this study, we aimed to improve the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RLX), a BCS class II drug, using a self-microemulsifying drug delivery system (SMEDDS). Based on the solubilities of RLX, Capryol 90, Tween 80/Labrasol ALF, and polyethylene glycol 400 (PEG-400) were selected as the oil, surfactant mixture, and cosurfactant, respectively. Pseudo-ternary phase diagrams were constructed to determine the optimal composition (Capryol 90/Tween 80/Labrasol ALF/PEG-400 in 150/478.1/159.4/212.5 volume ratio) for RLX-SMEDDS with a small droplet size (147.1 nm) and stable microemulsification (PDI: 0.227). Differential scanning calorimetry and powder X-ray diffraction of lyophilized RLX-SMEDDS revealed the loss of crystallinity, suggesting a molecularly dissolved or amorphous state of RLX in the SMEDDS formulation. Moreover, RLX-SMEDDS exhibited significantly higher saturation solubility and dissolution rate in water, simulated gastric fluid (pH 1.2), and simulated intestinal fluid (pH 6.8) than RLX powder. Additionally, oral administration of RLX-SMEDDS to female rats resulted in 1.94- and 1.80-fold higher area under the curve and maximum plasma concentration, respectively, than the RLX dispersion. Collectively, our findings suggest SMEDDS is a promising oral formulation to enhance the therapeutic efficacy of RLX.
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