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Title: Encapsulation and controlled release of rapamycin from polycaprolactone nanoparticles prepared by membrane micromixing combined with antisolvent precipitation
Authors: Othman, Rahimah
Vladisavljevic, Goran T.
Nagy, Zoltan K.
Holdich, R.G.
Keywords: Rapamycin
Nanoparticles
Membrane micromixing
Precipitation
Controlled drug release
Issue Date: 2016
Publisher: © American Chemical Society
Citation: OTHMAN, R. ... et al, 2016. Encapsulation and controlled release of rapamycin from polycaprolactone nanoparticles prepared by membrane micromixing combined with antisolvent precipitation. Langmuir, 32 (41), pp. 10685-10693.
Abstract: Rapamycin loaded polycaprolactone nanoparticles (RAPA-PCL NPs) with a polydispersity index of 0.006−0.073 were fabricated by anti-solvent precipitation combined with micromixing using a ringed stainless steel mem-brane with 10-μm diameter laser-drilled pores. The organic phase composed of 6 g L−1 of PCL and 0.6−3.0 g L-1 of RAPA in acetone was injected through the membrane at 140 L m−2 h−1 into 0.2 wt% aqueous polyvinyl alcohol solution stirred at 1300 rpm, resulting in a Z-average mean of 189−218 nm, a drug encapsulation efficiency of 98.8−98.9 % and a drug loading in the NPs of 9−33 %. The encapsulation of RAPA was confirmed by UV‐Vis spectroscopy, XRD, DSC, and ATR-FTIR. The disappearance of sharp characteristic peaks of crystalline RAPA in the XRD pattern of RAPA-PCL NPs revealed that the drug was molecularly dispersed in the polymer matrix or RAPA and PCL were present in individual amorphous domains. The rate of drug release in pure water was negligible due to low aqueous solubility of RAPA. RAPA-PCL NPs released more than 91 % of their drug cargo after 2.5 h in the release medium composed of 0.78−1.5 M of the hydrotropic agent N,N-diethylnicotinamide, 10 vol% of ethanol, and 2 vol% of Tween 20 in phosphate buffered saline. The dissolution of RAPA was slower when the drug was embedded in the PCL matrix of the NPs than dispersed in the form of pure RAPA nanocrystals.
Description: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Langmuir, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/acs.langmuir.6b03178
Sponsor: EPSRC grant EP/HO29923/1 and European Research Council grant [280106-CrySys]. Ministry of Higher Education Malaysia
Version: Accepted for publication
DOI: 10.1021/acs.langmuir.6b03178
URI: https://dspace.lboro.ac.uk/2134/22907
Publisher Link: http://dx.doi.org/10.1021/acs.langmuir.6b03178
ISSN: 0743-7463
Appears in Collections:Published Articles (Chemical Engineering)

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