Gupta Ankush, Singh Sima, Kotla Niranjan G, Webster Thomas J
Department of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.
Department of Chemical Engineering, Northeastern University, Boston, MA, USA ; Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah, Saudi Arabia.
Int J Nanomedicine. 2014 Dec 24;10:171-82. doi: 10.2147/IJN.S70449. eCollection 2015.
A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. One of the best options for successful drug delivery to the affected area of skin is the use of elastic vesicles (niosomes) which can be transported through the skin through channel-like structures. In this study, a combination of tretinoin (keratolytic agent) and benzoyl peroxide (BPO) (a potent antibacterial) was given by using niosomes as promising carriers for the effective treatment of acne by acting on a pathogenic site. In this section, niosomal gel formulation encapsulated drugs have been evaluated for in vitro, ex vivo, and in vivo, for their predetermined characteristics; and finally the stability of the niosome gel was tested at different temperature conditions for understanding of the storage conditions required for maintaining the quality of formulation attributes. The prepared niosome was found to be in the range of 531 nm with a zeta potential of -43 mV; the entrapment efficiencies of tretinoin (TRA) and BPO niosomes were found to be 96.25%±0.56% and 98.75%±1.25%, respectively. The permeated amount of TRA and BPO from the niosomal gel after 24 hours was calculated as 6.25±0.14 μg/cm(2) and 5.04±0.014 μg/cm(2), respectively. A comparative drug retention study in Wistar rat skin using cream, an alcoholic solution, and a niosomal gel showed 11.54 μg, 2.68 μg, and 15.54 μg amounts of TRA and 68.85 μg, 59.98 μg, and 143.78 μg amounts of BPO were retained in the layers of skin, respectively. In vivo studies of the niosomal gel and antiacne cream of TRA and BPO showed that the niosomal gel was more efficacious than the antiacne cream because niosomal gels with a 4.16-fold lower dose of BPO provided the same therapeutic index at targeted sites in comparison to the antiacne cream.
像痤疮这样的皮肤病非常常见，通常每个人一生中至少会患一次。角质层的结构常被比作砖墙，角质形成细胞被细胞间脂质薄片的“灰浆”所包围。将药物成功递送至皮肤患处的最佳选择之一是使用弹性囊泡（非离子型表面活性剂囊泡），其可通过类似通道的结构穿过皮肤。在本研究中，维甲酸（角质溶解剂）和过氧化苯甲酰（BPO，一种强效抗菌剂）联合使用非离子型表面活性剂囊泡作为有前景的载体，通过作用于致病部位来有效治疗痤疮。在本节中，已对包封药物的非离子型表面活性剂囊泡凝胶制剂进行了体外、离体和体内的预定特性评估；最后在不同温度条件下测试了非离子型表面活性剂囊泡凝胶的稳定性，以了解维持制剂质量属性所需的储存条件。制备的非离子型表面活性剂囊泡直径在531 nm范围内，ζ电位为 -43 mV；维甲酸（TRA）和BPO非离子型表面活性剂囊泡的包封率分别为96.25%±0.56%和98.75%±1.25%。24小时后，TRA和BPO从非离子型表面活性剂囊泡凝胶中的渗透量分别计算为6.25±0.14 μg/cm²和5.04±0.014 μg/cm²。在Wistar大鼠皮肤上使用乳膏、醇溶液和非离子型表面活性剂囊泡凝胶进行的药物保留对比研究表明，皮肤层中保留的TRA量分别为11.54 μg、2.68 μg和15.54 μg，BPO量分别为68.85 μg、59.98 μg和143.78 μg。TRA和BPO的非离子型表面活性剂囊泡凝胶和抗痤疮乳膏的体内研究表明，非离子型表面活性剂囊泡凝胶比抗痤疮乳膏更有效，因为与抗痤疮乳膏相比，BPO剂量低4.16倍的非离子型表面活性剂囊泡凝胶在靶向部位提供了相同的治疗指数。
