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This study aims to enhance the solubility of Olaparib, classified as biopharmaceutical classification system (BCS) class IV due to its low solubility and bioavailability using a solid self-nanoemulsifying drug delivery system (S-SNEDDS). For this purpose, SNEDDS formulations were created using Capmul MCM as the oil, Tween 80 as the surfactant, and PEG 400 as the co-surfactant. The SNEDDS formulation containing olaparib (OLS-352), selected as the optimal formulation, showed a mean droplet size of 87.0 ± 0.4 nm and drug content of 5.53 ± 0.09%. OLS-352 also demonstrated anticancer activity against commonly studied ovarian (SK-OV-3) and breast (MCF-7) cancer cell lines. Aerosil® 200 and polyvinylpyrrolidone (PVP) K30 were selected as solid carriers, and S-SNEDDS formulations were prepared using the spray drying method. The drug concentration in S-SNEDDS showed no significant changes (98.4 ± 0.30%, 25℃) with temperature fluctuations during the 4-week period, demonstrating improved storage stability compared to liquid SNEDDS (L-SNEDDS). Dissolution tests under simulated gastric and intestinal conditions revealed enhanced drug release profiles compared to those of the raw drug. Additionally, the S-SNEDDS formulation showed a fourfold greater absorption in the Caco-2 assay than the raw drug, suggesting that S-SNEDDS could improve the oral bioavailability of poorly soluble drugs like olaparib, thus enhancing therapeutic outcomes. Furthermore, this study holds significance in crafting a potent and cost-effective pharmaceutical formulation tailored for the oral delivery of poorly soluble drugs.
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http://dx.doi.org/10.1208/s12249-024-02927-2 | DOI Listing |
Pharm Dev Technol
July 2025
Department of Pharmaceutical Quality Assurance, KLE College of Pharmacy, Belagavi, KLE Academy of Higher Education and Research, Belagavi, Karnataka, India.
Darunavir, a nonpeptidic protease inhibitor, remains a cornerstone of antiretroviral therapy due to its potent activity against wild-type human immunodeficiency virus (HIV). However, its poor aqueous solubility and limited oral bioavailability, characteristic of Biopharmaceutical Classification System Class II drugs, restrict therapeutic efficacy, with an absorption rate of only 37%. To address these pharmacokinetic limitations, nanotechnology-based strategies have been explored to enhance drug solubility, systemic exposure, and targeted tissue distribution.
View Article and Find Full Text PDFPharm Dev Technol
July 2025
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.
This study developed a hydroxypropyl methylcellulose acetate succinate (HPMCAS)-functionalized supersaturated self-nanoemulsifying drug delivery system (HPMCAS-SNEDDS@BA) to address the poor solubility and bioavailability of baicalin (BA), a flavonoid with anti-colitis efficacy. The formulation was systematically optimized through solubility screening, emulsification efficiency evaluation, and pseudo-ternary phase diagram analysis. Central composite design-response surface methodology (CCD-RSM) was employed to identify the optimal SNEDDS@BA composition, followed by HPMCAS ratio optimization based on supersaturation maintenance in biorelevant media.
View Article and Find Full Text PDFPharm Dev Technol
June 2025
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.
Abiraterone acetate (ABT) is an androgen biosynthesis inhibitor approved for the treatment of prostate cancer. However, the treatment course of ABT is constrained by its high dose, poor solubility and permeability issues. A solid supersaturated self-nanoemulsifying drug delivery system (ssSNEDDS) is an excellent approach for improving drug loading.
View Article and Find Full Text PDFACS Omega
April 2025
Department of Pharmacology, Orotta College of Medicine and Health Sciences, Asmara University, Asmara, Eritrea.
The main purpose of this study was to design and develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) for the oral administration of benidipine (BD) and telmisartan (TEL) using the adsorption method with eucalyptus oil, Transcutol P, and Kolliphor EL via the Box-Behnken design approach. The prepared SNEDDS formulations were characterized using FTIR, DSC, SEM, and PXRD techniques and evaluated for zeta potential, refractive index, drug concentration, resistance to dilution, viscosity, and thermodynamic stability. Additionally, and stability studies were conducted.
View Article and Find Full Text PDFInt J Nanomedicine
April 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia.
Purpose: The inherent chemical instability of ramipril (RMP) can lead to reduced therapeutic efficacy and safety, emphasizing the need for innovative formulation strategies for increased stability and bioavailability. This study aims to develop RMP-loaded liquid and solid self-nanoemulsifying formulations (SNEDDSs) that incorporate cardioprotective black seed oil (BSO) as a natural source of bioactive thymoquinone (THQ) for comprehensive chemical stability and pharmacokinetic evaluation.
Methods: A systematic approach was employed to transform liquid SNEDDSs into both single-layer (Single-SNEPs) and multilayer (Multi-SNEPs) self-nanoemulsifying pellets through fluid bed coating technology.