Characterization and microbiological evaluation of chitosan-alginate microspheres for cefixime vaginal administration. (15th July 2018)

• Record Type: Journal Article
• Authors: Maestrelli, F.; Jug, M.; Cirri, M.; Kosalec, I.; Mura, P.
• Is Part Of: Carbohydrate polymers. Volume 192(2018)
• Page Start: 176
• Page End: 183
• Publication Date: 2018-07-15
• Subjects: Sodium alginate (PubChem CID: 5102882) -- Calcium alginate (PubChem CID: 44630049) -- Chitosan (PubChem CID: 21896651) -- Cefixime (PubChem CID: 5362065) -- 2, 3, 5-triphenyl-tetrazolium chloride (PubChem CID: 9283); Chitosan -- Alginate -- Microspheres -- Vaginal delivery -- Mucoadhesion -- Cefixime; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2018.03.054
• Languages: English
• ISSNs: 0144-8617

Abstract

Highlights: A cefixime vaginal formulation was developed based on chitosan-alginate microspheres. Entrapped amount increased with loading amount up to an optimal drug:polymer ratio. Swelling properties, drug entrapped amount and release rate were directly related. Microspheres loaded with 30 mg/mL drug showed the best water uptake and release rate. Microspheres loaded with 30 mg/mL drug showed the highest activity against E. coli . Abstract: Chitosan-alginate microspheres (MS) were developed for cefixime vaginal administration, to overcome problems associated with its oral administration. The effect of increasing drug-loading amount, by keeping the chitosan-alginate content constant, was investigated. Mucoadhesion studies indicated that all formulations assured in situ permanence longer than 2 h. Entrapment efficiency increased with drug loading concentration in the starting solution, reaching a plateau at 30 mg/mL indicative of the achievement of an optimal drug-to-polymer ratio. MS swelling properties increased with the entrapped drug amount, and, interestingly, water-uptake reached its maximum value at the same drug loading concentration of 30 mg/mL. The relationship found between MS water-uptake and drug release rate confirmed MS prepared with 30 mg/mL cefixime as the best formulation. Microbiological studies showed a relation between cefixime release rate from MS and Escherichia coli viability reduction, definitely indicating the selected MS formulation as the best for an effective local treatment of urogenital infections.