Characterization of various deformable liposomes with metronidazole.
Summary of "Characterization of various deformable liposomes with metronidazole."
Objective: The aim of this study was to investigate various deformable liposomes for their potential application for the vaginal administration of metronidazole. Materials and methods: Deformable liposomes composed of egg phosphatidylcholine (EPC) and various surfactants [sodium deoxycholate (SDCh), Tween 80 or Span 80] and conventional liposomes consisting of EPC and egg phosphatidylglycerol-sodium (EPG-Na) were prepared with and without metronidazole. Additionally, a freeze-thaw method was applied to both classes of vesicles (liposomes) containing the drug to improve its trapping capacity. All of the liposomes prepared were characterized and compared in terms of size, polydispersity, zeta potential, entrapment efficiency and their permeability on a Caco-2 cell monolayer. Results and discussion: Conventional liposomes, both with and without metronidazole, were larger than the deformable vesicles. The presence of ethanol in the preparations of the elastic EPC/SDCh and EPC/Tween 80 liposomes was found to affect the particle size in terms of reducing this parameter. Different types of vesicles were compared for their trapping efficiency of metronidazole and the highest entrapment was observed with conventional liposomes. However, deformable EPC/SDCh liposomes were found to enhance the permeability of metronidazole more effectively than the conventional liposomes based on the in vitro model of the epithelial barrier. Conclusion: These preliminary data indicate that EPC/SDCh liposomes may have a promising future in vaginal delivery of metronidazole. Therefore, additional investigations on elastic vesicles and their incorporation in a suitable vehicle should be considered to further evaluate their applicability in vaginal drug delivery.
Affiliation
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb , Zagreb , Croatia.
Journal Details
This article was published in the following journal.
Name: Drug development and industrial pharmacy
ISSN: 1520-5762
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22455377
- DOI: http://dx.doi.org/10.3109/03639045.2012.670247
Medical and Biotech [MESH] Definitions
Genotype
The genetic constitution of the individual; the characterization of the genes.
Unilamellar Liposomes
Single membrane vesicles, generally made of PHOSPHOLIPIDS.
Metronidazole
A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS. It has also been proposed as a radiation sensitizer for hypoxic cells. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985, p133), this substance may reasonably be anticipated to be a carcinogen (Merck, 11th ed).
Dimyristoylphosphatidylcholine
A synthetic phospholipid used in liposomes and lipid bilayers for the study of biological membranes.
Population Characteristics
Qualities and characterization of various types of populations within a social or geographic group, with emphasis on demography, health status, and socioeconomic factors.
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