EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY
Objective: The formulation effective delivery vehicle for anticancer drug is challenging owing to their low aqueous solubility. Their clinically acceptable formulations comprises of toxic solubilizers to solubilize the drug which evokes toxic and allergic reactions upon administration, Lipid based nanocarriers like liposomes and SLN have been explored as potential vehicles for improving delivery aspects of lipophilic drugs. In the present study paclitaxel loaded stearically stabilized emulsomes are prepared with the aim to provide non-toxic and biocompatible carriers with high Ptx loading efficiency.
Method: The formulations were prepared by modified solvent evaporation method using compritol as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/compritol ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein.
Results: The emulsomes so formed were uniform in size with mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulation showed pH dependent drug release with slow and sustained release profile. Slower drug release was observed from stearically stabilized emulsomes than the plain emulsomes. The drug release profile followed Higuchi model with Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption.
Conclusion: The stearically stabilized emulsome can serv.;es as novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water soluble drug as well.
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