Formulation, Optimization, and Characterization of Diclofenac SMEDDS and Incorporation into Self - Micro emulsifying Mouth Dissolving Films

Authors

  • Priyanka D. Borude
  • Disha
  • Sachin V. Kotwal

DOI:

https://doi.org/10.63682/jns.v13i1.9529

Keywords:

N\A

Abstract

Background: Diclofenac is a potent non-steroidal anti-inflammatory drug (NSAID) with poor water solubility and gastrointestinal (GI) side effects. Conventional oral diclofenac can have delayed onset and cause GI irritation. Self-micro emulsifying drug delivery systems (SMEDDS) improve solubility of hydrophobic drugs, while oral fast-dissolving films enhance convenience and speed of administration. Combining these approaches may yield rapid, efficient diclofenac delivery. Objectives: To formulate and optimize a diclofenac-loaded SMEDDS for improved solubility and absorption, incorporate it into a self-micro emulsifying mouth dissolving film (SMMDF), and evaluate the formulation’s in vitro characteristics and in vivo performance. Materials and Methods: Solubility of diclofenac was determined in various oils, surfactants, and co-surfactants to select SMEDDS components. Pseudo-ternary phase diagrams were constructed to identify self-emulsification regions. SMEDDS formulations were prepared and optimized using a mixture design to minimize droplet size. The optimized SMEDDS was characterized for droplet size, polydispersity index (PDI), zeta potential, and self-emulsification time. SMMDFs were prepared by solvent casting of polymer matrices containing the optimized SMEDDS. Films were evaluated for uniformity, mechanical properties, disintegration time, in vitro dissolution, and morphology. An in vivo pharmacokinetic study in rats compared the SMMDF to a conventional diclofenac tablet. Results: The optimized SMEDDS (oil: Capryol 90, surfactant: Tween 80, co-surfactant: Transcutol-HP) had a droplet size ~50 nm, PDI 0.22, and zeta potential –15 mV. SMMDFs were uniform (thickness ~100 μm) with high drug content (>98%) and fast disintegration (~25 s). In vitro, SMMDF released >90% of diclofenac in 5 min versus ~60% from a tablet. In rats, SMMDF showed higher C_max (4.1 vs 2.3 μg/mL) and shorter T_max (0.5 h vs 2 h) than the tablet, with a 1.6-fold increase in AUC, indicating significantly improved bioavailability (p<0.01). Conclusions: The diclofenac SMMDF achieved rapid dissolution and enhanced systemic exposure compared to the conventional formulation. This novel combination of SMEDDS with a mouth dissolving film offers a promising strategy for improving the onset and efficacy of poorly soluble drugs like diclofenac while potentially reducing GI side effects.

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Published

2024-10-24

How to Cite

1.
D. Borude P, Disha D, V. Kotwal S. Formulation, Optimization, and Characterization of Diclofenac SMEDDS and Incorporation into Self - Micro emulsifying Mouth Dissolving Films. J Neonatal Surg [Internet]. 2024 Oct. 24 [cited 2025 Dec. 16];13(1):1664-7. Available from: https://www.jneonatalsurg.com/index.php/jns/article/view/9529

Issue

Vol. 13 (2024): Journal of Neonatal Surgery

Section

Original Article

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