Abstract
Purpose. To design liposome-loaded microspheres, which release theliposomes in a time-controlled manner and in intact form.
Methods. Liposomes were encapsulated in biodegradabledextran-based microspheres, which were prepared using an aqueous two phasesystem consisting of poly(ethylene glycol) and methacrylated dextran.The effects of liposome size and membrane fluidity, microsphere watercontent, degree of methacrylate substitution, and type of dextranderivative used, on encapsulation efficiency, release, and integrity of theliposomes were investigated.
Results. Liposomes were entrapped in dextran-based microspheresquantitatively and with full preservation of their integrity. Liposomeswith a low, as well as with a high membrane fluidity, were releasedfrom the microspheres in their intact form and with preservation oftheir size. Release kinetics depended only on the degradation rate ofthe microspheres. For rapidly degrading systems, pulsed release wasobserved and the time after which the pulse occurred (from 5 until 25days) could be tailored by the gel characteristics such as initial watercontent, degree of methacrylate substitution, and type of hydrolyticallysensitive spacer present in the cross-links. This delay time was notdependent on the size of the liposomes in the range studied(0.1–0.2 μm). Microspheres which degraded more slowly showed, after a certaindelay time, sustained release of the liposomes extended up to 100 days.
Conclusions. A novel drug delivery concept based on the encapsulationof liposomes in biodegradable dextran-based microspheres wasdesigned. The system released the liposomes in intact form in acontrolled way after a prolonged period of time.
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Stenekes, R.J.H., Loebis, A.E., Fernandes, C.M. et al. Controlled Release of Liposomes from Biodegradable Dextran Microspheres: A Novel Delivery Concept. Pharm Res 17, 664–669 (2000). https://doi.org/10.1023/A:1007526114744
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DOI: https://doi.org/10.1023/A:1007526114744