Abstract

Background: Liposome offers many advantages over conventional dosage forms, like increased bioavailability, possibility of releasing drug at slower and constant rate, accurate drug release. Docetaxel is approved by the FDA for the treatment of locally advanced or metastatic breast cancer, head and neck cancer, gastric cancer. Docetaxel is BCS Class 4 drug; hence efficacy can be improved with liposomal formulation.
 Objectives: The Present study prepared Docetaxel loaded liposomal formulation.
 Materials and Methods: Formulation batches were designed on the basis of solvent, lipid to cholesterol ratio, lipid to release modifier ratio, hydration temperature and various physicochemical and morphological properties of formulation were examined. The zeta potential, particle size determination, pH, stability, determination of encapsulation efficacy, morphology of formulation and in-vitro drug release were investigated.
 Results: The zeta potential values of FD5 and FD9 were found to be -12.6 to -12.9 mV and -10.6 to -11.9 mV respectively. The entrapment efficiency of formulations of batch FD5 and FD9 were found to be 83.20% and 85.22% respectively. By comparing both FD5 and FD9 it was found that FD9 batch is optimized than FD5 in all aspects. The formulation batch FD9 has particle size of 105 nm, zeta potential in range of -10.6 to -11.9 mV; Drug entrapment efficiency 85.22%, Assay of formulation was 99.56 % and FD9 formulation shows extended release of Drug up to 13 hours.
 Conclusion: The study confirmed that the Liposome formulation was successfully prepared and evaluated.

Highlights

  • Liposomes were discovered by Alec D Bangham during the 1960s at the Babraham Institute, University of Cambridge, and comprise of single or different concentric lipid bilayers encapsulating an aqueous compartment [1,2]

  • Docetaxel is BCS Class 4 drug; efficacy can be improved with liposomal formulation

  • Materials and Methods: Formulation batches were designed on the basis of solvent, lipid to cholesterol ratio, lipid to release modifier ratio, hydration temperature and various physicochemical and morphological properties of formulation were examined

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Summary

Introduction

Liposomes were discovered by Alec D Bangham during the 1960s at the Babraham Institute, University of Cambridge, and comprise of single or different concentric lipid bilayers encapsulating an aqueous compartment [1,2]. The first formulation was made natural lipids; at present they can incorporate regular and manufactured lipids and surfactants. They have the capacity of ensnaring both lipophilic and hydrophilic agent, in the lipid layer and in the aqueous core, respectively. Throughout the previous 50 years liposomes have been broadly examined and they keep on being the subject of extraordinary research. They are esteemed for their natural and technological advantages delivery systems for biologically active substances, both in vitro and in vivo, and are viewed as the best drugcarrier system known to date [4]. The entrapment efficiency of formulations of batch FD5 and FD9 were

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