title: Polymeric microparticles-based formulation for the eradication of cutaneous candidiasis: development and characterization.
abstract: Cutaneous candidiasis is a common topical fungal infection which may be more prominent in patients associated with AIDS. It is usually treated by conventional formulations such as cream, gel, which show various adverse effects on skin along with systemic absorption. To overcome these drawbacks, various novel drug delivery systems have been explored. Poly(lactic-co-glycolic acid) (PLGA)-based microparticulate systems have shown good dermal penetration after topical application. Therefore, in the present study clotrimazole-loaded PLGA microspheres were prepared for targeted dermal delivery. Microspheres were prepared by using a single emulsification (oil-in-water, O/W) evaporation technique and characterized for different parameters. Prepared microparticulate systems were dispersed in Carbopol 934® gel and antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed guinea pigs. Particle size of optimized formulation was 2.9 µm along with 74.85% entrapment of drug. Skin retention studies revealed that drug accumulation in the skin was higher with microspheres gel as compared to marketed gel. Confocal microscopy of skin further confirmed penetration of microspheres up to 50 µm into the dermal region. In-vivo antifungal activity studies demonstrated that microsphere gel showed better therapeutic activity, lowest number of cfu/ml was recorded, as compared to marketed gel after 96 h of application. Based on the results of the study, it can be concluded that PLGA microparticles may be promising carriers to deliver clotrimazole intradermally for the treatment of invasive fungal infections.
authors.affiliation: Department of Pharmaceutics .
authors.forename: Lalit
authors.initials: L
authors.lastname: Kumar
authors.forename: Shivani
authors.initials: S
authors.lastname: Verma
authors.forename: Sumit
authors.initials: S
authors.lastname: Jamwal
authors.forename: Shubha
authors.initials: S
authors.lastname: Vaidya
authors.forename: Bhuvaneshwar
authors.initials: B
authors.lastname: Vaidya
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002179:Candidiasis, Cutaneous / Q000188:drug therapy*; D003022:Clotrimazole / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016503:Drug Delivery Systems; D005782:Gels / Q000737:chemistry; D006168:Guinea Pigs; D019344:Lactic Acid / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012867:Skin / Q000378:metabolism / Q000382:microbiology*
chemical_list: D000935:Antifungal Agents; D005782:Gels; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D003022:Clotrimazole