title: β-cyclodextrin nanosponges as multifunctional ingredient in water-containing semisolid formulations for skin delivery.
abstract: A β-cyclodextrin nanosponge cross-linked with pyromellitic dianhydride (βNS-PYRO) is reported for the first time as multifunctional ingredient in semisolid formulations for drug delivery to the skin. The role of βNS-PYRO on solubilization and stabilization of the photosensitizer benzoporphyrin-derivative monoacid ring A (BPDMA) and all-trans retinoic acid (atRA) as well as its effect on skin permeation of diclofenac (DIC) was investigated. Aqueous solutions, gels, and cream-gels were prepared from mixtures of βNS-PYRO with a conventional gelling agent at specific ratios. The incorporation of BPDMA in βNS-PYRO water solutions prevented its aggregation and gave kinetically stable complexes with high photostability and singlet oxygen generation upon irradiation. atRA incorporated in the βNS-PYRO-containing gel demonstrated a remarkable stability as compared with the formulation without βNS-PYRO, resulting in an eightfold increase of its lifetime. Skin permeation studies highlighted that βNS-PYRO in gels and cream-gels containing DIC significantly decreased the amount of drug permeated through the skin while increasing its amount in stratum corneum and viable epidermis. Overall, swellable βNS-PYRO turns to be a multifunctional coingredient with potential in topical monophasic and biphasic formulations to stabilize light-sensitive drugs and to localize the action of highly penetrating drugs in the external layers of skin.
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Napoli 80131, Italy.
authors.forename: Claudia
authors.initials: C
authors.lastname: Conte
authors.affiliation: Department of Chemistry, University of Torino, Torino 10125, Italy.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Caldera
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Napoli 80131, Italy.
authors.forename: Ovidio
authors.initials: O
authors.lastname: Catanzano
authors.affiliation: Di.S.T.A.Bi.F, Second University of Napoli, Caserta 81100, Italy.
authors.forename: Ivana
authors.initials: I
authors.lastname: D'Angelo
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Napoli 80131, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: Ungaro
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Napoli 80131, Italy.
authors.forename: Agnese
authors.initials: A
authors.lastname: Miro
authors.affiliation: Department of Chemistry, State University of Maringá, Maringá 87020-900, Brazil.
authors.forename: Diogo Silva
authors.initials: DS
authors.lastname: Pellosi
authors.affiliation: Department of Chemistry, University of Torino, Torino 10125, Italy. Electronic address: francesco.trotta@unito.it.
authors.forename: Francesco
authors.initials: F
authors.lastname: Trotta
authors.affiliation: Drug Delivery Laboratory, Department of Pharmacy, University of Napoli Federico II, Napoli 80131, Italy. Electronic address: quaglia@unina.it.
authors.forename: Fabiana
authors.initials: F
authors.lastname: Quaglia
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry*; D010539:Permeability; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013552:Swine; D014867:Water / Q000737:chemistry*; D047392:beta-Cyclodextrins / Q000008:administration & dosage* / Q000737:chemistry*
chemical_list: D005782:Gels; D047392:beta-Cyclodextrins; D014867:Water; C031215:betadex
keywords: biomaterials; complexation; cyclodextrins; skin; solubility; stability