Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process

International Journal of Pharmaceutics
Taekun AnSung-Joo Hwang

Abstract

Risperidone-loaded poly (D,L-lactide-co-glycolide) (PLGA) microspheres were prepared with a suspension-evaporation process with an aqueous suspension containing an in situ-formed aluminum hydroxide inorganic gel (SEP-AL process) and evaluated for encapsulation efficiency, particle size, surface morphology, glass transition temperature, in vitro drug release profile, and in vivo behavior. The SEP-AL microspheres were compared with conventional oil-in-water (O/W) emulsion solvent evaporation method using polyvinylalcohol (PVA) as an emulsifier (CP-PVA process). The microspheres were spherical in shape. DSC measurements showed that risperidone crystallinity was greatly reduced due to the homogeneous distribution of risperidone in PLGA microspheres. In vitro drug release profile from the microspheres showed a sigmoidal pattern of negligible initial burst up to 24h and minimal release (time-lag) for 7 days. After the lag phase, slow release took a place up to 25 days and then rapid release occurred sharply for 1 week. In vivo rat pharmacokinetic profile from the microspheres showed very low blood concentration level at the initial phase (up to 24h) followed by the latent phase up to 21 days. At the 3rd week, main phase started and t...Continue Reading

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Citations

May 24, 2020·Current Pharmaceutical Design·Ece Ö BülbülNeslihan Ü Okur
Feb 16, 2021·Journal of Microencapsulation·Luis Peña IcartLuís Maurício T R Lima
Nov 18, 2020·Advanced Drug Delivery Reviews·Christian Isalomboto NkangaFarshad Ramazani
May 26, 2021·Drug Development and Industrial Pharmacy·Bangqing WuLi Deng
Jun 9, 2021·Molecular Pharmaceutics·Ze Qiang ZhaoXin Dong Guo
Jan 16, 2021·ACS Biomaterials Science & Engineering·Jin Yoo, You-Yeon Won

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