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Polymers 2015, 7(6), 1145-1176; doi:10.3390/polym7061145

A Novel Melt-Dispersion Technique for Simplistic Preparation of Chlorpromazine-Loaded Polycaprolactone Nanocapsules

1
Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown 2193, South Africa
2
Department of Neurology, Division of Neurosciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown 2193, South Africa
3
Department of Neurosurgery, Division of Neurosciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown 2193, South Africa
*
Author to whom correspondence should be addressed.
Academic Editor: Cyrille Boyer
Received: 20 April 2015 / Revised: 5 June 2015 / Accepted: 8 June 2015 / Published: 19 June 2015
(This article belongs to the Special Issue Polymers and Polymeric Nanoparticles for Therapy and Imaging)

Abstract

The aim of this study was to design, synthesize and optimize chlorpromazine hydrochloride (CPZ)-loaded, poly-ε-caprolactone (PCL) based nanocapsules, intended for site specific delivery to the frontal lobe, using a novel melt-dispersion technique that is non-arduous, inexpensive and devoid of any hazardous organic solvents. Experimental trials using a central composite design were performed on 13 statistically derived formulations of various combinations of PCL (1000–3000 mg) and Polysorbate 80 (2%–5% v/v) on the physicochemical and physicomechanical properties and interactive effects on PCL nanocapsule formulation. Differential scanning calorimetry (DSC), Temperature modulated differential scanning calorimetry (TMDSC) and Fourier transform infrared spectroscopy (FTIR) revealed that there was no thermodegardation of the constituents utilized in the melt dispersion technique. Nanocapsule yields achieved were very high however entrapment of CPZ proved to be relatively low due to the highly hydrophilic nature of CPZ and the processing of the nanocapsules post synthesis. Nanocapsule sizes were in the nanotherapeutic range and varied from 132.7 ± 6.8 nm to 566.6 ± 5.5 nm. Zeta potential ranged from 15.1 ± 0.65 mV to 28.8 ± 0.84 mV revealing capsules that were of incipient to moderate stability. Transmission electron microscopy revealed nanocapsules that were spherical shape, well individualized with a moderate degree of flocculation. In vitro CPZ release was biphasic for all formulations with an initial burst release followed by pseudo-steady controlled release over 30 days. The cytotoxicity of the optimized nanocapsule system on a PC12 neuronal cell line proved to be minimal. Following incorporation of the optimized nanocapsules within a polymeric membrane, in vivo implantation of the device in a New Zealand Albino rabbit model proved the efficacy of the system in achieving prolonged more targeted CPZ levels to the brain. Extensive in vitro testing and optimization and preclinical evaluation supports the application for the use and feasibility of the CPZ-loaded, PCL based nanocapsules for the long-term management of certain psychotropic disorders where the benefits of nanotechnology can be exploited. View Full-Text
Keywords: neurotherapy; chlorpromazine hydrochloride; poly-ε-caprolactone; Polysorbate 80; melt-dispersion technique; nanocapsules; central composite design neurotherapy; chlorpromazine hydrochloride; poly-ε-caprolactone; Polysorbate 80; melt-dispersion technique; nanocapsules; central composite design
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Govender, T.; Choonara, Y.E.; Kumar, P.; Du Toit, L.C.; Modi, G.; Naidoo, D.; Pillay, V. A Novel Melt-Dispersion Technique for Simplistic Preparation of Chlorpromazine-Loaded Polycaprolactone Nanocapsules. Polymers 2015, 7, 1145-1176.

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