Novel preparation method for sustained-release PLGA microspheres using water-in-oil-in-hydrophilic-oil-in-water emulsion

Abstract

Xiaoyun Hong,1,2,* Liangming Wei,3,* Liuqing Ma,2 Yinghui Chen,4 Zhenguo Liu,1 Weien Yuan2,* 1Department of Neurology, Xinhua Hospital affiliated to Shanghai JiaoTong University, School of Medicine, Shanghai, People's Republic of China; 2School of Pharmacy, Shanghai JiaoTong University, 3Key Laboratory for Thin Film and Microfabrication Technology, Ministry of Education, Research Institute of Micro/Nanometer Science and Technology, Shanghai JiaoTong University, Shanghai, People's Republic of China; 4Department of Neurology, Jinshan Hospital, Fudan University, Shanghai, People's Republic of China *These authors contributed equally to this work Abstract: An increasing number of drugs are needing improved formulations to optimize patient compliance because of their short half-lives in blood. Sustained-release formulations of drugs are often required for long-term efficacy, and microspheres are among the most popular ones. When drugs are encapsulated into microsphere formulations, different methods of preparation need to be used according to specific clinical requirements and the differing physicochemical characteristics of individual drugs. In this work, we developed a novel method for sustained-release drug delivery using a water-in-oil-in-hydrophilic oil-in-water (w/o/oh/w) emulsion to encapsulate a drug into poly(lactic-co-glycolic acid) (PLGA) microspheres. Different effects were achieved by varying the proportions and concentrations of hydrophilic oil and PLGA. Scanning electron and optical microscopic images showed the surfaces of the microspheres to be smooth and that their morphology was spherical. Microspheres prepared using the w/o/oh/w emulsion were able to load protein efficiently and had sustained-release properties. These results indicate that the above-mentioned method might be useful for developing sustained-release microsphere formulations in the future. Keywords: protein, microspheres, water-in-oil-in-hydrophilic oil-in-water emulsion, sustained-release