Sontakke Arun, Dighe Sayali, Sharma Reena, Yadav Vivek, Jain Sanyog
Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Punjab 160062, India.
Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Punjab 160062, India.
Int J Pharm. 2024 Apr 25;655:124026. doi: 10.1016/j.ijpharm.2024.124026. Epub 2024 Mar 20.
Apremilast (APR) is a potent anti-psoriatic agent that inhibits the phosphodiesterase 4 enzyme. Due to the poor oral bioavailability and associated systemic side effects the clinical applicability of APR has been constrained. Nanotechnology-based carrier system presents a novel option to increase the efficacy of the topical treatment of APR. The current investigation deals with the development of fatty acid-surfactant conjugate-based hybrid mixed micellar gel (HMMG) for the topical delivery of APR. The developed micelles exhibited an average size of 83.59 ± 4.46 nm, PDI of 0.239 ± 0.047, % entrapment efficiency of ∼ 94.78 ± 3.98 %, with % practical drug loading of ∼11.37 ± 3.14 %. TEM analysis revealed the spherical shape of micelles. The hybrid micelles were further loaded in a carbopol®934P gel base for ease of application. Ex vivo permeation study revealed enhanced permeation and ∼ 38-fold higher retention in deeper layers of skin from a hybrid micellar gel. In vivo, assessment demonstrated augmented efficacy of APR-HMMG as compared to 0.1 % betamethasone valerate. Also, APR-HMMG showed no sign of irritation, suggesting superior safety as a topical application. Thus, the proposed formulation strategy represents a viable avenue for enhancing the therapeutic efficacy of various anti-psoriatic moieties.
阿普司特（APR）是一种强效的抗银屑病药物，可抑制磷酸二酯酶4。由于口服生物利用度差以及相关的全身副作用，阿普司特的临床应用受到限制。基于纳米技术的载体系统为提高阿普司特局部治疗的疗效提供了一种新选择。目前的研究涉及开发基于脂肪酸-表面活性剂共轭物的混合胶束凝胶（HMMG）用于阿普司特的局部递送。所制备的胶束平均粒径为83.59±4.46 nm，多分散指数为0.239±0.047，包封率约为94.78±3.98%，实际载药量约为11.37±3.14%。透射电镜分析显示胶束呈球形。为便于应用，将混合胶束进一步负载于卡波姆934P凝胶基质中。体外渗透研究表明，混合胶束凝胶的渗透增强，在皮肤深层的滞留量提高了约38倍。在体内，评估表明与0.1%戊酸倍他米松相比，阿普司特-HMMG的疗效增强。此外，阿普司特-HMMG没有显示出刺激迹象，表明作为局部应用具有更高的安全性。因此，所提出的制剂策略是提高各种抗银屑病药物治疗效果的可行途径。
