PMID: 2110539May 1, 1990Paper

Enzymatically activated microencapsulated liposomes can provide pulsatile drug release

FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology
P G KibatR Langer

Abstract

A system for the delayed or pulsed release of biologically active substances was achieved by encapsulating liposomes containing the substance of interest inside microcapsules. The microcapsules retain the liposomes but allow controlled diffusion of the active substance when it is released from the liposomes. Furthermore, by coating the liposomes with phospholipase A2 (an enzyme that removes an acyl group from the 2 position of phospholipids) before placing them within the microcapsule, a pulsatile release pattern was achieved both in vitro and in vivo. The time of onset of the pulse as well as the release rate can be controlled by the amount of phospholipase A2, the molecular weight of the poly(L-lysine) that is used to coat the microencapsulated liposomes, and the composition of the phospholipid bilayer membrane. Even at 37 degrees C the system would protect a model enzyme (horseradish peroxidase). When not placed inside the microencapsulated liposomes, the enzyme lost its activity in solution at 37 degrees C in a few days, whereas it retained 40% of the initial activity after 30 days of incubation at 37 degrees C inside the microencapsulated liposomes.

Citations

Apr 15, 2011·Journal of Drug Delivery·Maluta S MufamadiValence M K Ndesendo
Mar 13, 2010·Journal of Biomedical Materials Research. Part B, Applied Biomaterials·Chengtie WuYin Xiao
Apr 8, 2010·Science Translational Medicine·Yihai Cao, Robert Langer
Jan 1, 1998·Drug Delivery·N Venkatesan, S P Vyas
May 27, 2011·Journal of the Royal Society, Interface·Chengtie WuGianaurelio Cuniberti
Oct 1, 2011·Chemical Communications : Chem Comm·Michael E Hahn, Nathan C Gianneschi
Feb 18, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·A KikuchiT Okano
Feb 15, 2003·Journal of Pharmaceutical Sciences·Nikhil O Dhoot, Margaret A Wheatley
Mar 18, 1991·Biochimica Et Biophysica Acta·S CohenR Langer
Aug 30, 2013·Langmuir : the ACS Journal of Surfaces and Colloids·Matthew B DowlingSrinivasa R Raghavan
Sep 28, 1990·Science·R Langer

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