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The Thai Journal of Pharmaceutical Sciences

Abstract

Paclitaxel is an antineoplastic drug, effective for various complex cancers especially ovarian and breast cancer. Due to its high hydrophobicity, an adjuvant such as polyethoxylated castor oil (Cremophor EL) has to be used in its clinical administration; however, it causes serious side-effects. Inclusion of paclitaxel in lipid matrix (lipospheres) has been proved to be a good approach to eliminate the need for Cremophor EL and to prolong the release of the drug. This paper describes the development of lipospheres as carriers for paclitaxel. Lipospheres constituted of bioacceptable and biodegradable lipids were fabricated and characterised. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR), and X-ray diffraction techniques (XRD) and in vitro release studies were employed to characterise the fabricated lipospheres for size and size distribution, surface morphology, thermodynamic property and crystallinity and study the release pattern. The in vitro anti-tumoral activity of the developed lipospheres was assessed using U373 cancer cell lines. The in vitro release behaviour of paclitaxel from the developed lipospheres exhibited a biphasic pattern characterised by an initial fast release during the first 24 h, followed by a slower and continuous release. The results were more pronounced after incubation for prolonged time due to slow diffusion of drug from lipospheres. Our results demonstrate that incorporation of paclitaxel in lipospheres shows comparable cytotoxicity to pristine paclitaxel. Hence, the developed formulation can be used for activity against complex cancers.

DOI

10.56808/3027-7922.3320

First Page

117

Last Page

130

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