Fabrication of core–shell PLGA/PLA–pNIPAM nanocomposites for improved entrapment and release kinetics of antihypertensive drugs--颗粒学报PARTICUOLOGY

Basu, T., Pal, B., & Singh, S. (2018). Fabrication of core–shell PLGA/PLA–pNIPAM nanocomposites for improved entrapment and release kinetics of antihypertensive drugs. Particuology, 40, 169-176. https://doi.org/10.1016/j.partic.2017.10.002

Fabrication of core–shell PLGA/PLA–pNIPAM nanocomposites for improved entrapment and release kinetics of antihypertensive drugs

Tanushree Basu, Bonamali Pal, Satnam Singh ^*

School of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala 147004, Punjab, India

10.1016/j.partic.2017.10.002

Volume 40, October 2018, Pages 169-176

Received 14 April 2017, Revised 6 October 2017, Accepted 13 October 2017, Available online 3 February 2018, Version of Record 28 July 2018.

E-mail: ssingh@thapar.edu

Highlights

• Core–shell PLA/PLGA–pNIPAM nanoparticles were synthesized as a biocompatible drug carrier.

• Ramipril-loaded PLGA–pNIPAM core–shell NPs exhibited higher entrapment efficiency (78%) than PLA.

• Up to 96% sustained release over 24 h in PBS medium was achieved for PLGA–pNIPAM NPs.

• Ramipril release from PLGA–pNIPAM core–shell NPs was diffusion controlled.

Abstract

Polylactic acid (PLA) and poly(lactic-co-glycolic) acid (PLGA) are two commonly applied biodegradable polymers for the preparation of nanocomposites used in drug-delivery systems. However, these polymers lack desirable attributes such as resistance to aggregation during long-term storage due to lyophilisation. To improve their efficacy, in this work, PLA and PLGA were encapsulated within a shell of poly(N-isopropylacrylamide) (pNIPAM) using a single emulsion technique followed by an aqueous free radical precipitation polymerisation process, yielding core–shell PLA/PLGA–pNIPAM nanocomposites. The nanocomposites were characterised using zeta potential, dynamic light scattering, and transmission electron microscopy analyses and were further applied as a delivery system for ramipril, an antihypertensive drug. The drug-loaded PLGA–pNIPAM core–shell nanoparticles exhibited a higher drug content (91%) and entrapment efficiency (78%) than their PLA counterparts. An in vitro release study of the formulations at pH 7.3 in phosphate-buffered saline indicated that PLGA was more efficient than PLA with a sustained release of 86% of ramipril from the polymer matrix within 24 h. Furthermore, to determine the release kinetics, the data were fitted to Korsmeyer–Peppas and Higuchi models; the release of ramipril from the polymer matrix followed zero-order rate kinetics and an anomalous (non-Fickian) diffusion mechanism.

Graphical abstract

Keywords

Poly(lactic-co-glycolic) acid; Polylactic acid; Poly(N-isopropylacrylamide); Antihypertensive drug; Entrapment efficiency; Drug release

文章导读