In Vivo Evaluation of Tazarotene Solid Lipid Nanoparticles Gel for Topical Delivery

Abstract

The purpose of this research work was to develop and optimize the Solid Lipid Nanoparticles (SLNs) of Tazarotene for the effective topical delivery in the treatment of psoriasis. Tazarotene loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s design and based on the results further investigation was made using central composite design. The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, TEM, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F1) was found to be 98.12 ± 1.52%, whereas pure drug release was 42.12 after 60 min. The optimized formulation was incorporated into the gel. The release rate (flux) of tazarotene across the membrane and excised skin differs significantly. The accumulative amount of Tazarotene in skin from SLN based gel formulation and marketed gel were 41.12 ± 0.12 mg and 30.02 ± 0.04 mg respectively. This result supported our hypothesis made in skin permeation studies on rat skin. From histopathological studies the microscopic observations indicate that the optimized SLN formulation, SLN based gel formulation and marketed gel has no significant effect on the microscopic structure of the skin. The skin-irritation studies indicated that SLN based gel containing Tazarotene did not show any sign of skin irritation as compared to moderate erythema shown by marketed gel formulation (Tazret® gel) after 72 h of application. Thus, SLN based gel formulation demonstrated advantage over marketed formulation in improving the skin tolerability of Tazarotene indicating their potential in improving patient acceptance and topical delivery of Tazarotene.

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“…Lipids have been proposed as an alternative carrier to overcome the limitations of polymeric nanoparticles, especially for lipophilic pharmaceuticals. The formulation of Luliconazole as solid lipid nanoparticles also increases the drug's efficacy and exhibits a better therapeutic action 13,1 . Luliconazole-It is an antifungal agent belonging to imidazole group, which has a broad spectrum antifungal activity and has been shown to be effective against a wide range of fungi, especially dermatophytes.…”

“…Rheological parameters, in-vitro drug release, and permeation tests were carried out on the SLNbased gels. In-vitro antifungal studies revealed that an SLN-based drug was more effective in inhibiting the growth of Candida albicans and had a sustained release drug profile, implying that it could be used to treat topical fungal infections 13 . Shilpa N. Shrotriya et al, 2017 worked on Silybinloaded stable lipid nanoparticle-enhanced gel formulation and development for irritant contact dermatitis.…”

Nanocarriers as Active Ingredients Enhancers in the Cosmetic Industry—The European and North America Regulation Challenges

“…Solid lipid nanoparticles (SLNs) are biodegradable lipids with low toxicity [ 22 , 92 ] that can not only protect the constituents they incorporate from destruction, but can also be used as a means of transporting cosmetic agents into the stratum corneum since they can easily penetrate this layer [ 64 , 93 ]. SLNs can entrap various active compounds with several properties such as hydrophilic [ 94 ], lipophilic [ 95 ], or poorly water-soluble [ 96 ]. Furthermore, SLNs have better stability than liposomes as a result of being solid [ 97 ].…”

“…The preparation method and physicochemical characteristics of the active agents can influence the efficiency of SLNs [ 100 ]. A study by Aland et al [ 96 ] demonstrated that a transdermal delivery formulation of tazarotene loaded into SLNs had better tolerability than the marketed formulation for the treatment of psoriasis. Indeed, the new formulation did not reveal any sign of skin irritation, showing an improvement in transdermal delivery of tazarotene.…”

Topical Solid Lipid Nanoparticles Based Gel of Lavender Essential Oil for Anti‑inflammatory Activity

“…Add 2-3 drops of triethanolamine. As soon as, the triethanolamine is added the solution turns viscous and gel is formed [11].…”