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In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives

Acta Pharmaceutica Sinica B 2021年第8期11卷 2469-2487页

作者： Yanping Huang Qin Yu Zhongjian Chen Wei Wu Quangang Zhu Yi Lu Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China

lipid-based formulations(LBFs)have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble ***,construction of in vitro and in vivo correlations(IVIVCs)for LBFs is quite challenging,owing to a complex in vivo processing of these *** this paper,we start with a brief introduction on the gastrointestinal digestion of lipid/LBFs and its relation to enhanced oral drug absorption;based on the concept of IVIVCs,the current status of in vitro models to establish IVIVCs for LBFs is reviewed,while future perspectives in this field are *** vitro tests,which facilitate the understanding and prediction of the in vivo performance of solid dosage forms,frequently fail to mimic the in vivo processing of LBFs,leading to inconsistent *** vitro digestion models,which more closely simulate gastrointestinal physiology,are a more promising *** some successes in IVIVC modeling,the accuracy and consistency of these models are yet to be validated,particularly for human data.A reliable IVIVC model can not only reduce the risk,time,and cost of formulation development but can also contribute to the formulation design and optimization,thus promoting the clinical translation of LBFs.

关键词： lipid-based formulation In vitro and in vivo correlations Lipolysis Absorption Oral delivery Model In silico prediction Perspectives

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Enhanced intestinal lymphatic absorption of saquinavir through supersaturated self-microemulsifying drug delivery systems

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Asian Journal of Pharmaceutical Sciences 2020年第3期15卷 336-346页

作者： Kanghee Jo Hyeongmin Kim Prakash Khadka Taejun Jang Soo Jin Kim Seong-Ha Hwang Jaehwi Lee College of Pharmacy Chung-Ang UniversitySeoul 06974Republic of Korea

The therapeutic potential of saquinavir, a specific inhibitor of human immunodeficiency virus(HIV)-1 and HIV-2 protease enzymes, has been largely limited because of a low solubility and consequnt low bioavailability. Thus, we aimed to design a supersaturated selfmicroemulsifying drug delivery system(S-SMEDDS) that can maintain a high concentration of saquinavir in gastro-intestinal fluid thorugh inhibiting the drug precipitation to enhance the lymphatic transport of saquinavir and to increase the bioavailability of saquinavir considerably. Solubilizing capacity of different oils, surfactants, and cosurfactants for saquinavir was evaluated to select optimal ingredients for preparation of *** the construction of pseudo-ternary phase diagram, SMEDDS formulations were established. A polymer as a precipitation inhibitor was selected based on its viscosity and drug precipitation inhibiting capacity. The S-SMEDDS and SMEDDS designed were administered at an equal dose to rats. At predetermined time points, levels of saquinavir in lymph collected from the rats were assessed. SMEDDS prepared presented a proper selfmicroemulsification efficiency and dispersion stability. The S-SMEDDS fabricated using the SMEDDS and hydroxypropyl methyl cellulose 2910 as a precipitation inhibitor exhibited a signficantly enhanced solubilizing capacity for saquinavir. The drug concentration in a simulated intestinal fluid evaluated with the S-SMEDDS was also maintained at higher levels for prolonged time than that examined with the SMEDDS. The S-SMEDDS showed a considerably enhanced lymphatic absoprtion of saquinavir in rats compared to the ***, the S-SMEDDS would be usefully exploited to enhance the lymphatic absorption of hydrophobic drugs that need to be targeted to the lymphatic system.

关键词： Lymphatic drug delivery Self-microemulsifying drug delivery system Saquinavir Precipitation inhibitor Supersaturation lipid-based formulation

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Oral lipid-based drug delivery systems–an overview

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Acta Pharmaceutica Sinica B 2013年第6期3卷 361-372页

作者： Sandeep Kalepu Mohanvarma Manthina Veerabhadhraswamy Padavala Department of Pharmaceutical Technology Shri Vishnu College of PharmacyBhimavaram 534202Andhra PradeshIndia

The formulation of drugs is carried out with the principle objective of enhancing their *** water soluble drugs are challenging for the formulation scientists with regard to solubility and ***-based drug delivery systems(LBDDS)are one of the emerging technologies designed to address such *** or solubilizing the drug in lipid excipients can lead to increased solubilization and absorption,resulting in enhanced *** advances in these formulation technologies have led to the successful commercialization of lipidbased *** review provides a comprehensive summary and characterization of lipid-based formulations,especially for oral delivery,from both physicochemical and biopharmaceutical *** review also focuses on the processing techniques necessary to obtain solid lipid-based formulations for oral delivery,along with a brief discussion of lipid excipients and their characterization.

关键词： lipid-based formulation lipid excipient Solubilization Lymphatic absorption

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