<p>Although acne is not life-threatening, it does impact patients’ psychological health dramatically. Tazarotene (TZ), a topical retinoid anti-acne drug, usually causes side effects like peeling and irritation. Therefore, TZ is an excellent candidate for topical nanocarriers to reduce those side effects and boost patients’ compliance. TZ-loaded transfersomes (TZ-Ts) were prepared and characterized by percentage entrapment efficiency (EE), particle size (PS), zeta potential (ZP), amount of TZ released after 8 h (Q8h), and polydispersity index determinations. Different statistical methodologies were adopted to optimize TZ-Ts. Optimized TZ-Ts formulation (OTT) was morphologically inspected and incorporated into a gel. At this point of the research, the optimized TZ cubosomes formulation (OTC) from our previous work was also incorporated into a gel for the in vivo comparative assessment of both nanosystem gels in the acne inflammatory murine model. Results analysis and numerical optimization resulted in a positively charged OTT with desirable EE, Q8h, and PS. OTT possessed EE of 94.1%, PS of 501.4 nm, ZP of + 66.1 mV, and Q8h of 77.3%. Regarding their anti-acne activity, OTC-gel outperformed OTT-gel and the market product Acnitaz®. Both gels reduced the irritating effect of Acnitaz®. This research represents a good application of nanocarriers’ merit in therapeutic activity enhancement.</p> Graphical Abstract <p></p>

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Optimized Tazarotene Transfersomes Versus Previously Optimized Tazarotene Cubosomes: Exploring Their In Vivo Anti-Acne Activity in a Cutibacterium acnes Inflammatory Murine Model

  • Doaa Hegazy,
  • Nazek M. Fayed,
  • Hanzada T. Nour El-Din,
  • Basant Ahmed Habib,
  • Randa Tag Abdelrehim

摘要

Although acne is not life-threatening, it does impact patients’ psychological health dramatically. Tazarotene (TZ), a topical retinoid anti-acne drug, usually causes side effects like peeling and irritation. Therefore, TZ is an excellent candidate for topical nanocarriers to reduce those side effects and boost patients’ compliance. TZ-loaded transfersomes (TZ-Ts) were prepared and characterized by percentage entrapment efficiency (EE), particle size (PS), zeta potential (ZP), amount of TZ released after 8 h (Q8h), and polydispersity index determinations. Different statistical methodologies were adopted to optimize TZ-Ts. Optimized TZ-Ts formulation (OTT) was morphologically inspected and incorporated into a gel. At this point of the research, the optimized TZ cubosomes formulation (OTC) from our previous work was also incorporated into a gel for the in vivo comparative assessment of both nanosystem gels in the acne inflammatory murine model. Results analysis and numerical optimization resulted in a positively charged OTT with desirable EE, Q8h, and PS. OTT possessed EE of 94.1%, PS of 501.4 nm, ZP of + 66.1 mV, and Q8h of 77.3%. Regarding their anti-acne activity, OTC-gel outperformed OTT-gel and the market product Acnitaz®. Both gels reduced the irritating effect of Acnitaz®. This research represents a good application of nanocarriers’ merit in therapeutic activity enhancement.

Graphical Abstract