Drug release from injectable depots: two different in vitro mechanisms

Journal of Controlled Release : Official Journal of the Controlled Release Society
Liwei WangLothar Kleiner

Abstract

Certain poly (lactide-co-glycolide) (PLGA)/benzyl benzoate (BB) solutions can form gels when injected into buffer (depot formation) as well as upon ageing under ambient conditions. When evaluating various PLGAs in benzyl benzoate, we have found that only those that gel upon ageing also form gel depots in buffer. This indicates that depot formation in this system may be fundamentally different from the phase inversion depot formation that has been observed for PLGA in water-miscible solvents. The drug release kinetics in vitro is controlled both by diffusion and erosion, with the base form of the drug being always released faster than its salt form. This is due to base-catalyzed hydrolysis. While gel permeation chromatography (GPC) measurements show a continuous decrease in molecular weight, the rheological properties upon buffer injection show maxima, for the base drug and the salt drug. The location of the viscosity maximum with time is dependent on the nature of the drug and its concentration.

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Citations

Oct 2, 2009·Pharmaceutical Research·Karin SchoenhammerAchim Goepferich
Jan 1, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Raghu Raj Singh ThakurDavid S Jones
Apr 25, 2014·AAPS PharmSciTech·Hatim AliSomnath Singh
Jun 29, 2012·Journal of Drug Targeting·Wei Li Lee, Say Chye Joachim Loo
Dec 29, 2013·Drug Development and Industrial Pharmacy·Muge KilicarslanRoland Bodmeier
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Jul 1, 2012·Drug Discovery Today. Technologies
May 1, 2012·Journal of Controlled Release : Official Journal of the Controlled Release Society·Sabine Kempe, Karsten Mäder
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Nov 26, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ying ZhaoTianwei Tan
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Jun 13, 2012·The Journal of Pharmacy and Pharmacology·Jie Shen, Diane J Burgess
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Aug 8, 2021·Advanced Drug Delivery Reviews·Xiaoyi Wang, Diane J Burgess

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