Naslov
Mucoadhesive microspheres for vaginal administration of Cefixime:development and evaluation

Autori
Maestrelli, Francesca ; Jug, Mario ; Kosalec, Ivan ; Cirri, Marzia ; Mura, Paola

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Book of Abstracts / Mandić, Zoran - Zagreb : International Association of Physical Chemists (IAPC), 2017, 76-76

Skup
6th IAPC Meeting: Sixth World Conference on Physico-Chemical Methods in Drug Discovery & Third World Conference on ADMET and DMPK

Mjesto i datum
Zagreb, Hrvatska, 4.-7. rujna

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
cefixim, mucoadhesive microsphere, vaginal administration

Sažetak
Vagina is becoming a preferred route of drug administration, not only for local treatment of vaginal diseases, but also for systemic delivery, due to the benefits offered compared to the oral route, such as need of lower doses, less frequent administration, elimination of gastrointestinal disturbances and first-pass effect. Different innovative formulation strategies like the use of bioadhesive and/or thermosensitive polymers, micro- or nano-particulate systems have been proposed to improve drug vaginal delivery and absorption. Among these, mucoadhesive multiparticulate systems offer several advantages compared to conventional vaginal dosage forms, covering a wide mucosa area, assuring a prolonged in situ drug permanence and allowing a controlled and sustained drug release. We recently investigated the effectiveness of different mucoadhesive polymers for the development of microspheres (MS) for vaginal delivery of metronidazole ; among the different tested formulations, chitosan (CS) coated Ca-alginate MS covered gave the best results in terms of drug entrapment, mucoadhesion and antibacterial activity. Based on these premises, the goal of this work was the development of mucoadhesive CS-coated Ca-alginate MS for vaginal administration of cefixime (CFX), a third-generation cephalosporin antibiotic used in the treatment of urinary-tract infections and gonorrheia. Ca-alginate MSprepared by ionotropic gelation technique were submitted to different coating methods with CS and loaded with increasing CFX concentration. Each batch was characterized for drug entrapment, mean weight and diameter, morphology (by ESEM and optical microscopy), and mucoadhesion properties. Swelling and drug release studies showed a relationship between drug content in the beads and MS water uptake, allowing the choice of MS with the optimal drug/polymer ratio endowed with the best swelling and drug release profile. Microbiological studies showed a close relation between reduction of metabolic activity of E. Coli (taken as model strain) and drug release rate from MS, confirming the 300 mg CFX-loaded MS as the best formulation and proving its suitability for local treatment of vaginal diseases.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA