To enhance the solubility of Repaglinide, we attempted to use Plasdone S 630, a novel solubility enhancer. Followed by the hot-melt extrusion method and made into a tablet dosage form. The prepared dosage forms subjected to all pre-compression and post-compression parameters evaluations. The data obtained from in-vitro drug release suggested that the trial-11 is the ideal formulation among all other formulations. The in-vitro release was also profiling around 95% within 45 minutes. The hardness of the prepared tablets was around 10-12 kg/cm 2 with the friability was less than 1%. So, this method could apply on the regular basis for formulating the tablet dosage forms.
Background:
Paclitaxel (PTX) is a potent anticancer drug which is highly effective
against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer
drugs can enhance its toxicity against tumor cells at low concentrations.
Objective:
To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity
against cancerous cells.
Method:
The solubility of PTX was screened in various lipids. Solid lipid nanoparticles
of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire
44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized
for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and
in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance
toxicity towards cancerous cells was tested by performing cytoxicity assay in
MCF7 cell line.
Results:
Solubility studies of PTX in lipids indicated better solubility when Cutina HR
and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with
a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained
release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were
found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.
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