Encapsulation and controlled release of rapamycin from polycaprolactone nanoparticles prepared by membrane micromixing combined with antisolvent precipitation Othman et al.pdf (914.74 kB)

Encapsulation and controlled release of rapamycin from polycaprolactone nanoparticles prepared by membrane micromixing combined with antisolvent precipitation

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posted on 19.10.2016 by Rahimah Othman, Goran Vladisavljevic, Zoltan Nagy, Richard Holdich
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.

Funding

EPSRC grant EP/HO29923/1 and European Research Council grant [280106-CrySys]. Ministry of Higher Education Malaysia

History

School

  • Aeronautical, Automotive, Chemical and Materials Engineering

Department

  • Chemical Engineering

Published in

Langmuir: the ACS journal of surfaces and colloids

Volume

32

Issue

41

Pages

10685 - 10693

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.

Publisher

© American Chemical Society

Version

AM (Accepted Manuscript)

Publisher statement

This work is made available according to the conditions of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) licence. Full details of this licence are available at: https://creativecommons.org/licenses/by-nc-nd/4.0/

Acceptance date

30/09/2016

Publication date

2016-09-30

Notes

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

ISSN

0743-7463

eISSN

1520-5827

Language

en

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