Gel s liposomski uklopljenim kloramfenikolom: karakterizacija i oslobađanje in vitro

Scientific paper - Original scientific paper

• Title (english): Liposomal gel with chloramphenicol: Characterisation and in vitro release
• Author: Željka Pavelić
• Author: Nataša Škalko-Basnet
• Author: Ivan Jalšenjak
• Author's institution: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology)
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract (croatian)

Cilj ovog rada bio je priprava i razvoj liposomskog terapijskog sustava s uklopljenim kloramfenikolom namijenjenog lokalnoj terapiji bakterijskog vaginitisa. Kloramfenikol je uklopljen u liposome fosfolipidnog sustava fosfatidilkolin/fosfatidilglicerol (molarni omjer 9:1), priređene dvjema metodama, proliposomskom i metodom razrjeđenja poliola. Obje preparacije su uspoređene i liposomi su karakterizirani s obzirom na veličinu čestica, polidisperznost, te uspješnost uklapanja. Provedena su ispitivanja stabilnosti liposoma in vitro u medijima koji svojim pH i sastavom oponašaju humanu vaginalnu sluznicu (pufer pH 4.5 i umjetni vaginalni medij). Kako bi se postigla prikladna viskoznost pripravka i dodatno povećala stabilnost liposoma namijenjenih vaginalnoj primjeni, liposomi su umiješani u bioadhezivni gel pripravljen iz karbopola 974P NF. In vitro ispitivanja s liposomima uklopljenima u gel pokazala su produljeno oslobađanje uklopljenog kloramfenikola. Pritom se čak nakon 24 sata inkubacije u umjetnom vaginalnom mediju više od 40% početno uklopljenog kloramfenikola zadržalo u gelu. Ispitivanja stabilnosti liposoma u gelu tijekom skladištenja potvrdila su povoljan učinak gela na očuvanje početne raspodjele uklopljenih liposoma s obzirom na veličinu. Ispitivanja provedena u ovom radu potvrđuju mogućnost primjene liposoma kao novog terapijskog sustava u lokalnoj terapiji bakterijski vaginalnih infekcija.

Abstract (english)

The aim of our study was to develop a liposomal carrier system for the local treatment of bacterial vaginosis, capable to efficiently deliver entrapped drug during an extended period of time. Chloramphenicol was entrapped in liposomes composed of egg phosphatidylcholine/egg phosphatidylgycerol-sodium (9:1, molar ratio) and prepared by two different methods, the proliposome method and the polyol dilution method. Both liposome preparations were characterised and compared for particle size, polydispersity, entrapment efficiency and tested for in vitro stability in media that simulate human vaginal conditions (buffer pH 4.5 and vaginal fluid simulant). To achieve application viscosity of liposomes and to further improve their stability, liposomes prepared by the proliposome method were incorporated in the bioadhesive gel made of Carbopol 974P NF resin. In vitro release studies of liposomes incorporated in the gel have shown a prolonged release of entrapped chloramphenicol compared to control gel. Even after 24 hours of incubation in the vaginal fluid simulant, more than 40% of the originally entrapped drug was still retained in the gel. Storage stability studies have proven the ability of the Carbopol 974P NF gel to preserve the original size distribution of incorporated liposomes. All the performed experiments confirm the applicability of liposomes as a novel drug carrier system for the local treatment of bacterial vaginosis.

• Keywords (croatian): liposomi; kloramfenikol; bioadhezivni gel; stabilnost; vaginalna primjena
• Keywords (english): liposomes; chloramphenicol; bioadhesive gel; stability; vaginal application
• Language: croatian
• Language: english
• Publication type: Scientific paper - Original scientific paper
• Publication status: Published
• Peer review: Peer review - international
• Publication version: Published version
• Journal title: Acta Pharmaceutica
• Numbering: vol. 54, no. 4, pp. 319-330
• p-ISSN: 1330-0075
• e-ISSN: 1846-9558
• URN:NBN: urn:nbn:hr:163:926499
• Publication: 2004
• Document URL: https://hrcak.srce.hr/16907
• Type of resource: Text
• Access conditions: Open access
• Created on: 2020-04-09 14:15:51