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Preparation, characterization and in vivo pharmacodynamic evaluation of thymopentin loaded poly(lactide acid)/poly(lactide-co-glycolide acid) implants.

Abstract：

:To avoid the clinical inconvenience of repeated injection of the immune modulator thymopentin (TP5), biodegradable implants comprising a mixed polymer matrix of poly(lactide acid) (PLA) and poly(lactide-co-glycolide acid) (PLGA) were produced using a simple extrusion method. Drug release from these TP5-loaded implants was characterized both in vitro and in vivo. Pharmacodynamic studies were carried out in immunosuppressed rats using the ratio of CD4(+)/CD8(+) cells, determined by flow cytometry, as an index of immunity. The results indicated that the entrapment efficiency of the implants was greater than 98%, but the release rate of TP5 depended on the drug loading. Implants containing less than 10% TP5 showed consistent release over 30 days, with low burst-release both in vitro and in vivo. Improved immunity and survival rates were observed in rats treated by TP5 injection and in rats given middle-to-high dose implants. When the release of TP5 exceeded 0.1 mg/kg body weight/day the CD4(+)/CD8(+) ratios increased in the 3 weeks after implantation, reaching a maximum (91.6% of the normal level) by the end of the third week. The TP5-loaded implants presented here provide a promising alternative to injections and the results support the further development of controlled-release TP5 formulations.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Wei G,Jin L,Xu L,Liu Y,Lu W

doi

10.1016/j.ijpharm.2010.07.036

subject

Has Abstract

pub_date

2010-10-15 00:00:00

pages

123-9

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(10)00563-6

journal_volume

398

pub_type

杂志文章

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