Abstract
Doxorubicin loaded into liposomes grafted with polyethylene glycol (PEG) has been demonstrated to have a longer circulation time and lower cardiotoxicity than doxorubicin (DOX). This study aims to investigate the biophysical characterization of a marketed formulation DOX-encapsulated liposome (DOX-NPTM). The interactions between doxorubicin and liposomal lipids can help in liposomal development. The liposome and DOX-NPTM were characterized in terms of differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The rheological properties of liposomal samples were also measured. Physical interactions may be occurred between the drug functional groups and liposomal lipids, probably by weak hydrogen bond formation or weak bond formation due to dipole-dipole interaction. There was no shift of existing peaks or appearance of new peaks was detected between the characteristic peaks of the liposomal lipids were present in the DOX-encapsulated liposome sample. This suggests that there were physical interactions that took place only between the drug and lipids and no chemical interaction between them. DSC information shows that the phase transition temperature shifts to lower temperature degrees after loading of DOX into the liposomes. The DSC curve has a small broadening. This may infer a little cooperativity decrease between acyl chains of liposomal membranes after DOX inclusion. The encapsulation of DOX into liposomes decreases the plastic viscosity of liposomes (from 1.64 to 1.48 cP), which shows that the membrane fluidity was increased.
Highlights
A cytotoxic anthracycline derivative doxorubicin has some success when utilized as a chemotherapeutic in different human cancer forms
The liposomes are composed of hydrogenated soy phosphatidylcholine (HSPC),9.58 mg/ml; N-(carbonyl-ethoxypolyethylene glycol 2000) -1,2distearoyl-sn-glycero- 3-phospho- ethanolamine sodium salt (DPEG-DSPE), 3.19 mg/ml; cholesterol, 3.19 mg/ml, ammonium sulfate, approximately 2 mg/ml; histidine as a buffer and sucrose to maintain isotonicity
The Fourier transformer infrared radiation (FTIR) spectra of the liposome and DOX-NPTM samples have been shown in Fig (3.2)
Summary
A cytotoxic anthracycline derivative doxorubicin has some success when utilized as a chemotherapeutic in different human cancer forms. Its treatment has a cardiotoxicity as side-effect. Doxorubicin loaded into PEGylated liposomes has been approved to decrease cardiotoxicity and increase tumor localization [1]. These liposomes leads to increased accumulation within the skin and circulation times, limiting the drug release at the tumor site [2]. Liposomes may be defined as lipid (usually phospholipids) vesicles enclosing an aqueous space [3]. Liposomes are most frequently composed of phospholipids, phosphatidylcholine, but may include other lipids, such as egg phosphatidylethanolamine, when they are consistent with lipid bilayer structure [4,5]. A liposome design may employ surface ligands when attaching to unhealthy tissue [6]
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