Drug-nanoencapsulated PLGA microspheres prepared by emulsion electrospray with controlled release behavior.

Shenglian Yao,Shenglian Yao,Huiying Liu,Xiumei Wang,Yuanyuan Li,Yuanyuan Li,Luning Wang,Shukui Yu

doi:10.1093/rb/rbw033

Abstract

The development of modern therapeutics has raised the requirement for controlled drug delivery system which is able to efficiently encapsulate bioactive agents and achieve their release at a desired rate satisfying the need of the practical system. In this study, two kind of aqueous model drugs with different molecule weight, Congo red and albumin from bovine serum (BSA) were nano-encapsulated in poly (dl-lactic-co-glycolic acid) (PLGA) microspheres by emulsion electrospray. In the preparation process, the aqueous phase of drugs was added into the PLGA chloroform solution to form the emulsion solution. The emulsion was then electrosprayed to fabricate drug-nanoencapsulated PLGA microspheres. The morphology of the PLGA microspheres was affected by the volume ratio of aqueous drug phase and organic PLGA phase (Vw/Vo) and the molecule weight of model drugs. Confocal laser scanning microcopy showed the nanodroplets of drug phase were scattered in the PLGA microspheres homogenously with different distribution patterns related to Vw/Vo. With the increase of the volume ratio of aqueous drug phase, the number of nanodroplets increased forming continuous phase gradually that could accelerate drug release rate. Moreover, BSA showed a slower release rate from PLGA microspheres comparing to Congo red, which indicated the drug release rate could be affected by not only Vw/Vo but also the molecule weight of model drug. In brief, the PLGA microspheres prepared using emulsion electrospray provided an efficient and simple system to achieve controlled drug release at a desired rate satisfying the need of the practices.

Highlights

Controlled-release strategies allowed for drug delivery in a controllable pattern at a specific location and time present numerous advantages over conventional drug administration, such as prolonged therapeutic period, enhanced efficacy, reduced systemic toxicities, eliminated dosage and improved patient compliance [1,2,3]
The morphology of the PLGA microspheres was affected by the volume ratio of aqueous drug phase and organic PLGA phase (Vw/Vo) and the molecule weight of model drugs
BSA showed a slower release rate from PLGA microspheres comparing to Congo red, which indicated the drug release rate could be affected by Vw/Vo and the molecule weight of model drug

Summary

Introduction

Controlled-release strategies allowed for drug delivery in a controllable pattern at a specific location and time present numerous advantages over conventional drug administration, such as prolonged therapeutic period, enhanced efficacy, reduced systemic toxicities, eliminated dosage and improved patient compliance [1,2,3]. Polymeric DDS are easy to be fabricated, chemically modified and adjusted degradation rate and achieve long-term sustained drug release via physical encapsulation or chemical immobilization. Most importantly, they do not need surgical removal upon complete drug.

Methods

Results

Conclusion