Abstract

Background: The study was aimed to prepare and evaluate tamoxifen loaded controlled release liposomes to reduce the side effects of tamoxifen during cancer treatment. 
 Methods: Different tamoxifen loaded liposomes were prepared by modified ether injection (MEIM) and thin film hydration method (TFHM) under prescribed conditions. The prepared liposomes were characterized by using optical microscopy, evaluating encapsulation efficiency, in-vitro and ex-vivo diffusion studies by using dialysis membrane and chicken intestinal sac respectively.
 Results: The data revealed that all of the liposomes were spherical in shape and stable under three physical conditions i.e. 4, 25 and 37 ± 2°C temperatures and 60 ±5% relative humidity. Additionally most of the liposomes followed zero order and class II release kinetics. It was also observed that with the increase of phospholipids and cholesterol, entrapment efficiency of liposome vesicles increased thus giving a controlled release drug delivery system but further increase reduced this efficiency at a certain level.
 Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment.

Highlights

  • Tamoxifen is used very commonly for the treatment of estrogen receptor positive breast cancer which is considered a pioneering drug because of its ubiquitous application in both treatment and chemoprevention of breast cancer [1] and reduction of the chances of breast cancer in high-risk patients [2]

  • Whitfield et al has reported that tamoxifen has a relatively high biological half-life which is 5-7 days and 99% protein binding after administration which reduces the effectiveness of the drug

  • The liposomal formulation containing tamoxifen were prepared by modified ether injection method (MEIM) and thin film hydration method (TFHM) using phosphatidylcholine and cholesterol with the purpose of evaluating the effect of phospholipids and cholesterol and their different level on physical and structural properties of liposomes

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Summary

Introduction

Tamoxifen is used very commonly for the treatment of estrogen receptor positive breast cancer which is considered a pioneering drug because of its ubiquitous application in both treatment and chemoprevention of breast cancer [1] and reduction of the chances of breast cancer in high-risk patients [2]. It is generally administered through oral and parenteral route to treat patients but several potential problems arise uniquely because of the use of oral therapy and oncologists need to be aware about the drug interactions and bioavailability of tamoxifen [3]. Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment

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