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Effect of medium-chain triglycerides on the release behavior of Endostar encapsulated PLGA microspheres.

Abstract：

:The incomplete release of Endostar from PLGA microspheres was observed in our previous study. In the present study, we focused on the effect of medium-chain triglycerides (MCT) on the in vitro/in vivo release behavior of Endostar encapsulated PLGA microspheres, which were prepared by a water-in-oil-in-water (W/O/W) double-emulsion method with or without MCT. The in vitro accumulated release of Endostar from microspheres co-encapsulated with 30% MCT was found to be 79.04% after a 30-day incubation period in PBS (pH 7.4) at 37 degrees C. However, the accumulated release of Endostar from MCT-free microspheres was found to be only 32.22%. Pouches containing Endostar encapsulated PLGA microspheres were implanted subcutaneously in rats. The effect of MCT on the in vivo release showed a similar trend to the in vitro release. After 30 days, only 9.87% of the total encapsulated Endostar was retained in microspheres co-encapsulated with 30% MCT, while 42.25% of Endostar was retained in MCT-free microspheres. The co-encapsulation of MCT provided the microspheres with a porous surface, which significantly improved the in vitro/in vivo release of Endostar from PLGA microspheres. In addition, in vitro experiments showed that MCT co-encapsulated PLGA microspheres had more inter-connected pores, faster degradation of PLGA, and faster swelling of microspheres, which helped to explain the mechanism of the effect of MCT on improving the release of Endostar from PLGA microspheres.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Meng B,Li L,Hua S,Wang Q,Liu C,Xu X,Yin X

doi

10.1016/j.ijpharm.2010.07.018

subject

Has Abstract

pub_date

2010-09-15 00:00:00

pages

136-43

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(10)00545-4

journal_volume

397

pub_type

杂志文章

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