ABSTRACT
Liposomes incorporating sodium deoxycholate (NaDC) were prepared by the method of reverse phase evaporation and used for drug delivery by the oral route. Hexamethylmelamine (HMM), an anti-tumor agent, was chosen as a model drug and encapsulated into liposomes incorporating NaDC (NaDC-Lip). Several properties of NaDC-Lip containing HMM (HMM NaDC-Lip), such as particle size, entrapment efficiency, pinacyanol chloride (PIN) spectral characteristics with various molar ratio of NaDC/PC, as well as the vesicle stability measurements with calcein were evaluated. In vivo, the area under the plasma concentration-time curve obtained from the pharmacokinetics study of HMM NaDC-Lip was found to be approximately 9.76- and 1.21-fold higher than that of HMM solution and HMM Lip, respectively, indicating that NaDC-Lip can be used as a potential carrier for oral drug administration.
Subject(s)
Altretamine/administration & dosage , Antineoplastic Agents, Alkylating/administration & dosage , Deoxycholic Acid/chemistry , Liposomes/chemistry , Administration, Oral , Altretamine/pharmacokinetics , Animals , Antineoplastic Agents, Alkylating/pharmacokinetics , Carbocyanines/chemistry , Cholesterol/chemistry , Chromatography, High Pressure Liquid , Drug Carriers , Drug Compounding , Drug Stability , Female , Fluoresceins/chemistry , Lipids/chemistry , Particle Size , Rats , Rats, Wistar , Spectrophotometry, UltravioletABSTRACT
BACKGROUND: Multivesicular liposomes (MVLs), uncoated and coated with N-trimethyl chitosan (TMC), have been studied for their potential use for drug delivery by the oral route. METHOD: Synthesized TMC was characterized by infrared spectroscopy, revealing the presence of trimethyl groups, and by proton nuclear magnetic resonance spectroscopy, allowing the calculation of the degree of substitution quaternization (70.2%). Oxymatrine (OM), a natural quinolizidine alkaloid used clinically for treating hepatitis B, was chosen as a model drug. The surface-modified MVLs and uncoated MVLs were characterized in vitro in terms of their shape, size, zeta potential, entrapment efficiency, coating efficiency, the stability of MVLs in polymer suspension, and the stability in simulated gastric and intestinal fluids. RESULTS: In vivo, the area under the plasma concentration-time curve obtained from the pharmacokinetics study of TMC-coated MVLs was found to be about 3.26- and 1.96-fold higher than that of OM solution and uncoated MVLs, respectively. CONCLUSION: TMC-coated MVLs can be considered as a potential carrier for oral drug administration.
