DEVELOPMENT OF ACECLOFENAC LOADED MICROSPONGE GELS: A STATISTICAL QUALITY BY DESIGN (QBD) APPROACH TOWARDS OPTIMIZATION AND EVALUATION

RAKHIMOL K.; PRAJITHA BIJU; SINDHOOR S. M.; NATASHA NAVAL AGGARWAL; SANDHYA V.; DEEKSHA RAI

doi:10.22159/ijap.2023v15i6.49122

Authors

RAKHIMOL K. Department of Pharmaceutics, College of Pharmacy Kannur Medical College, Kannur, Anjarakandy, India
PRAJITHA BIJU Department of Pharmaceutics, Yenepoya Pharmacy College and Research Centre, Karnataka-575018, Mangaluru, India https://orcid.org/0000-0001-8136-3943
SINDHOOR S. M. Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore-575018, Karnataka India https://orcid.org/0000-0003-3937-9858
NATASHA NAVAL AGGARWAL Department of Pharmaceutical Chemistry, Yenepoya Pharmacy College and Research Centre, Karnataka-575018, Mangaluru, India https://orcid.org/0000-0002-5464-8625
SANDHYA V. Department of Pharmaceutics, Yenepoya Pharmacy College and Research Centre, Karnataka-575018, Mangaluru, India https://orcid.org/0000-0002-6154-4023
DEEKSHA RAI Department of Pharmacognosy, Yenepoya Pharmacy College and Research Centre Deralakatte, Yenepoya Pharmacy College and Research Centre, Karnataka-575018, Mangaluru, India https://orcid.org/0000-0003-1495-4502

DOI:

https://doi.org/10.22159/ijap.2023v15i6.49122

Keywords:

Microsponge, Quassi emulsion technique, Quality by design, Ishikawa fishbone diagram, Gel

Abstract

Objective: The current research aims to deliver Aceclofenac in a controlled manner through a microsponges-loaded drug delivery system for the treatment of inflammation.

Methods: The formulations were prepared by the Quasi-emulsion solvent diffusion method and characterized for particle size and drug entrapment efficiency. For the optimization of the formulation through the Quality by Design (QbD) approach, Quality target product profiles (QTPP) were set up considering various key factors that affect the quality of the formulation. Further optimization of the important factors in relation to the major Critical Quality Attributes (CQAs) was conducted by applying full factorial design using the Design of Expert Software (11.0 software, Stat-Ease, Inc., USA). The optimized formulation was incorporated into the gel, and characterized for morphological analysis by Scanning Electron Microscopy (SEM), drug content, and ex-vivo permeation studies (DD solver, Version 2.0).

Results: It was found that process parameters such as drug-to-polymer ratio, the volume of the internal phase, and concentration of the emulsifier and polyvinyl alcohol (PVA), played a crucial role in improving the drug entrapment efficiency and particle size. On the other hand, stirring time did not significantly affect the particle size. Through Design of Expert (DOE) analysis, a PVA concentration of 0.641 mg/ml and an internal phase volume of 12.5 ml were identified to be the ideal concentrations to obtain the optimized microspongal gel formulation (MS4). Characterization studies were carried out on MS4, which displayed a drug encapsulation of 94%, with a C_max of 81.62 mg/ml, and a T_max of 12 h. Stability studies carried out as per the International Conference of Harmonization (ICH) guidelines confirmed no noticeable change in physical appearance and drug content.

Conclusion: Overall, this study focused on optimizing the formulation of microsponges for efficient dermal drug delivery, considering various critical variables and process parameters. The resulting optimized formulation demonstrated promising drug release and potential for the effective management of inflammation disorders.

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