Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies
Autor: | T.C. Beber, Ruy Carlos Ruver Beck, Diego Fontana de Andrade, M C Fontana, Maike Windbergs, Karine Coradini, Birthe Kann |
---|---|
Přispěvatelé: | Helmholtz Centre for infection research, Inhoffenstr. 7, 38124 Braunschweig, Germany. |
Rok vydání: | 2014 |
Předmět: |
Drug
Drug Liberation Polymers Surface Properties media_common.quotation_subject Drug Compounding Skin Absorption Sus scrofa Pharmaceutical Science In Vitro Techniques Vibration Dexamethasone Dermis Stratum corneum medicine Animals Tissue Distribution Particle Size Glucocorticoids media_common Skin Drug Carriers Chromatography Microscopy Confocal integumentary system Chemistry General Medicine Permeation medicine.anatomical_structure Spray drying Microscopy Electron Scanning Emulsions Particle size Drug carrier Biotechnology |
Zdroj: | European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V. 88(3) |
ISSN: | 1873-3441 |
Popis: | Topical glucocorticoids (TG) such as dexamethasone (DEX) have been used for decades for the treatment of skin diseases. However, TG present well-documented side effects and their delivery to the skin is often insufficient. Therefore, many efforts have been undergone to improve the amount of drug delivered to the skin and to reduce side effects at the same time. In this work, the feasibility of DEX-submicron polymeric particles (SP) prepared by vibrational spray-drying as an approach to overcome the challenges associated with the topical administration of this drug class was evaluated. DEX was homogeneously dispersed in the SP matrix, according to confocal Raman microscopy analysis. Drug-loaded SP were incorporated into the oil phase of oil-in-water emulsions (creams). The formulation containing polymeric submicron particles (C-SP) showed controlled drug release kinetics and a significant drug accumulation in skin compared to formulations containing non-polymeric particles or free drug. DEX accumulation in the stratum corneum was evaluated by tape stripping and a depot effect over time was observed for C-SP, while the formulation containing the free drug showed a decrease over time. Similarly, C-SP presented higher drug retention in epidermis and dermis in skin penetration studies performed on pig skin in Franz diffusion cells, while drug permeation into the receptor compartment was negligible. It was demonstrated, for the first time, the advantageous application of submicron polymeric particles obtained by vibrational spray-drying in semisolid formulations for cutaneous administration to overcome challenges related to the therapy with TG such as DEX. |
Databáze: | OpenAIRE |
Externí odkaz: |