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Microsponge Gel Approach to Increase the Stability and Efficacy of Avobenzone as a Sun-Protective Agent

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Abstract

Purpose

Avobenzone is a broad-spectrum sun-protective agent widely used in the form of creams and lotions. However, it is highly photo-unstable and causes irritation and systemic absorption which needs to be addressed. Microsponges are porous, polymeric carriers that are designed to deliver a pharmaceutical/cosmetic ingredient efficiently at the minimum dose and also to modify the drug release (sustained release) while reducing the skin toxicity problems pertaining to the drug. An attempt was made to formulate avobenzone-loaded microsponge gel.

Method

The microsponges for the delivery of avobenzone were successfully prepared by quasi-emulsion solvent diffusion method. The formulated microsponges were characterized for production yield, particle size, SEM, % entrapment efficiency, % drug release, FTIR and DSC. The optimized microsponges were further incorporated in hydrogel (HPMC K4M) in different ratios and evaluated for pH, viscosity, homogeneity, spreadability, stability testing, skin irritation study and sun protection factor (SPF) testing.

Results

The results showed that microsponge were spherical in shape with pore size in the range 0.10–0.30 μm. The production yield was between the range of 47 and 91.81%. The particle size was obtained within the range of 200 to 399 μm, indicating that increase in solvent (DCM) concentration reduces the particle size. Entrapment efficiency of formulation was ranging between 60 and 77.40%. In vitro drug release showed prolonged release of the drug for a duration of 8 h, and the % CDR was in the range of 27.79 to 65.66%. The microsponge gel showed good homogeneity and viscosity in the range of 1556 to 2622 cps, and spreadability was between 4.1 and 5.9 g.cm/s. The gel was found to be stable at 40 °C temperature and 75% RH, for a duration of 60 days. Microsponge gel was non-irritant on the rat skin and showed controlled release.

Conclusion

The controlled release and barrier effect of gel from microsponge result in prolonged retention of avobenzone along with decreased permeation activity. Hence, in conclusion, the study revealed enhanced efficacy and reduced toxicity with prolonged release of drug. It also showed better sun protection factor of 25 compared to the marketed preparation which was sun protection factor 20.

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Acknowledgements

The authors are also thankful to the Institute of KLE College of Pharmacy, Belagavi, for providing the facility for research work and also thankful for all the staff members and friends for their guidance throughout the research work.

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Authors and Affiliations

  1. Department of Pharmaceutics, KLE College of Pharmacy, KLE Academy of Higher Education and Research, Belagavi, Karnataka, India

    Ankita Patil, Rajashree S. Masareddy & Archana S. Patil

  2. Department of Pharmacology, KLE College of Pharmacy, KLE Academy of Higher Education and Research, Belagavi, Karnataka, India

    Prarambh S. R. Dwivedi

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  1. Ankita Patil
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Contributions

AKP performed the study and drafted the manuscript. RSM designed the protocol and reviewed the draft. ASP helped for FTIR and DSC. PSR helped AKP for the animal study.

Corresponding author

Correspondence to Rajashree S. Masareddy.

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Ethics Approval and Consent to Participate

This work included the use of twelve albino Wister rats which was accepted by the IAEC of KLE College of Pharmacy, Belagavi, Reg. No. 221/Po/Re/S/2000?CPCSEA in the meeting dated 13/03/2021, resolution No 30.

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The authors declare no competing interests.

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Patil, A., Masareddy, R.S., Patil, A.S. et al. Microsponge Gel Approach to Increase the Stability and Efficacy of Avobenzone as a Sun-Protective Agent. J Pharm Innov 17, 1347–1359 (2022). https://doi.org/10.1007/s12247-021-09616-8

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