2021•Dermatologic TherapyOpen access

Preparation and evaluation of adapalene nanostructured lipid carriers for targeted drug delivery in acne

Saman Ahmad Nasrollahi, Faezeh Koohestani, Atefeh Naeimifar, Aniseh Samadi, Alireza Vatanara, Alireza Firooz

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Abstract

Adapalene (ADA) is believed to be one of the topical treatments utilized commonly in case of acne. Nanostructured lipid carriers (NLCs) have been established as an effective carrier system with certain advantages, for instance increased solubility, drug targeting, controlled drug release, and stability of ADA. This study was conducted to obtain the formulation with a good therapeutic property. All formulations were formed by probe sonicator and its characterizations were analyzed. Finally, the therapeutic effects of 0.1% ADA-loaded nanostructured lipid carriers (NLC-ADA) were evaluated. This formulation had a great entrapment efficiency (EE) that illustrated a controlled drug release profile. A pilot clinical evaluation conducted on 15 patients (age 25.23 ± 12.24 years) with mild to moderate acne vulgaris lesions. The results demonstrated significant reduction in acne severity index and the number of inflammatory and noninflammatory lesions after 12 weeks of treatment (P-value .02, .04, and .01, respectively). Subjective results were confirmed with significant improvement in size and intensity of porphyrin production in pilosebaceous follicles (P-value = .03). The study demonstrated that the formulation was safe and revealed the proper improvement rate of acne lesions after 12 weeks.

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Adapalene (ADA) is believed to be one of the topical treatments utilized commonly in case of acne. Nanostructured lipid carriers (NLCs) have been established as an effective carrier system with certain advantages, for instance increased solubility, drug targeting, controlled drug release, and stability of ADA. This study was conducted to obtain the formulation with a good therapeutic property. All formulations were formed by probe sonicator and its characterizations were analyzed. Finally, the therapeutic effects of 0.1% ADA-loaded nanostructured lipid carriers (NLC-ADA) were evaluated. This formulation had a great entrapment efficiency (EE) that illustrated a controlled drug release profile. A pilot clinical evaluation conducted on 15 patients (age 25.23 ± 12.24 years) with mild to moderate acne vulgaris lesions. The results demonstrated significant reduction in acne severity index and the number of inflammatory and noninflammatory lesions after 12 weeks of treatment (P-value .02, .04, and .01, respectively). Subjective results were confirmed with significant improvement in size and intensity of porphyrin production in pilosebaceous follicles (P-value = .03). The study demonstrated that the formulation was safe and revealed the proper improvement rate of acne lesions after 12 weeks.

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Available abstract

Adapalene (ADA) is believed to be one of the topical treatments utilized commonly in case of acne. Nanostructured lipid carriers (NLCs) have been established as an effective carrier system with certain advantages, for instance increased solubility, drug targeting, controlled drug release, and stability of ADA. This study was conducted to obtain the formulation with a good therapeutic property. All formulations were formed by probe sonicator and its characterizations were analyzed. Finally, the therapeutic effects of 0.1% ADA-loaded nanostructured lipid carriers (NLC-ADA) were evaluated. This formulation had a great entrapment efficiency (EE) that illustrated a controlled drug release profile. A pilot clinical evaluation conducted on 15 patients (age 25.23 ± 12.24 years) with mild to moderate acne vulgaris lesions. The results demonstrated significant reduction in acne severity index and the number of inflammatory and noninflammatory lesions after 12 weeks of treatment (P-value .02, .04, and .01, respectively). Subjective results were confirmed with significant improvement in size and intensity of porphyrin production in pilosebaceous follicles (P-value = .03). The study demonstrated that the formulation was safe and revealed the proper improvement rate of acne lesions after 12 weeks.

Key concepts: Acne, Adapalene, Medicine, Drug, Therapeutic effect, Dermatology, Drug delivery, Drug carrier

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