Hydrogel containing dexamethasone-loaded nanocapsules for cutaneous administration: preparation, characterization, and in vitro drug release study

Drug Dev Ind Pharm. 2010 Aug;36(8):962-71. doi: 10.3109/03639041003598960.

Abstract

Context: Our group previously reported the development of dexamethasone-loaded polymeric nanocapsules as an alternative for topical dermatological treatments.

Objective: Our study aimed to prepare and characterize a hydrogel containing this system to improve the effectiveness of the glucocorticoid for cutaneous disorders.

Methods: For the antiproliferative activity assay, a dexamethasone solution and D-NC were tested on Allium cepa root meristem model. D-NC were prepared by the interfacial deposition of preformed polymer. Hydrogels were prepared using Carbopol Ultrez 10 NF, as polymer, and characterized according to the following characteristics: pH, drug content, spreadability, viscosity, and in vitro drug release.

Results and discussion: Nanocapsules showed mean particle size and zeta potential of 201 +/- 6 and -5.73 +/- 0.42 nm, respectively. They demonstrated a lower mitotic index (4.62%) compared to free dexamethasone (8.60%). Semisolid formulations presented acidic pH values and adequate drug content (between 5.4% and 6.1% and 100% and 105%, respectively). The presence of nanocapsules in hydrogels led to a decrease in their spreadability factor. Intact nanoparticles were demonstrated by TEM as well as by dynamic light scattering (mean particle size < 300 nm). In vitro studies showed a controlled dexamethasone release from hydrogels containing the drug associated to the nanocapsules following the Higuchi's squared root model (k = 20.21 +/- 2.96 mg/cm(2)/h(1/2)) compared to the hydrogels containing the free drug (k = 26.65 +/- 2.09 mg/cm(2)/h(1/2)).

Conclusion: Taking all these results together, the hydrogel containing D-NC represent a promising approach to treat antiproliferative-related dermatological disorders.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / analysis
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects
  • Chemical Phenomena
  • Dexamethasone / administration & dosage*
  • Dexamethasone / analysis
  • Dexamethasone / chemistry*
  • Dexamethasone / pharmacology
  • Diffusion
  • Drug Carriers / administration & dosage*
  • Drug Carriers / analysis
  • Drug Carriers / chemistry
  • Drug Carriers / pharmacology
  • Drug Compounding / methods
  • Hydrogels / chemical synthesis*
  • Hydrogels / chemistry*
  • Hydrogen-Ion Concentration
  • Immunosuppressive Agents / administration & dosage
  • Immunosuppressive Agents / analysis
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology
  • Meristem / cytology
  • Meristem / drug effects
  • Mitosis / drug effects
  • Nanocapsules / administration & dosage*
  • Nanocapsules / chemistry*
  • Onions / drug effects
  • Particle Size
  • Plant Roots / cytology
  • Plant Roots / drug effects
  • Solubility
  • Suspensions

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Hydrogels
  • Immunosuppressive Agents
  • Nanocapsules
  • Suspensions
  • Dexamethasone