Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, India.
J Liposome Res. 2011 Dec;21(4):324-32. doi: 10.3109/08982104.2011.575380. Epub 2011 May 31.
Exposure of skin to various chemical and physical agents results in excessive stress to the outermost cell layer of the skin, causing different degenerative effects that can be minimized by using antioxidant formulations. The major challenge, in this regard, is to develop a formulation, which can prevent photodegradation of the actives, thus allowing a significant amount to be deposited at the site. In recent decades, liposomal formulations have been extensively employed to overcome the barrier properties of the skin and photodegradation of actives. In the present study, chitosan-reduced gold nanoparticles were investigated for its potential as a carrier to prepare liposomes by a spray-drying method. Liposomes so obtained were characterized for phospholipid recovery, diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy, particle size, zeta potential, encapsulation efficiency, and deposition of drug and gold nanoparticles in the rat skin. Further, a liposomal gel formulation was prepared using Carbopol® 980 NF (Noveon Systems, Kochi, India) and evaluated for drug deposition in the skin. Antioxidant activity of vitamin C encapsulated in gold liposomes was determined on a human leukemia (HL-60) cell line. The use of gold nanoparticles as a carrier showed improved phospholipid recovery and thus overcomes the liposome scalability problem. DRIFT spectra confirmed the presence of phospholipid in the formulation. Liposomal gel showed improved drug deposition, as compared to control and marketed preparations. A more interesting contribution of the chitosan-reduced gold nanoparticles was an enhanced antioxidant activity seen in case of the vitamin C-loaded gold liposomal formulation. Liposomal formulation was found to be stable for 3 months at 30°C and 65% relative humidity.
皮肤暴露于各种化学和物理制剂会导致皮肤最外层细胞层承受过度压力，从而产生不同的退化效应，而使用抗氧化制剂可以最小化这些效应。在这方面的主要挑战是开发一种制剂，该制剂可以防止活性剂的光降解，从而允许大量活性剂沉积在作用部位。在最近几十年中，脂质体制剂已被广泛用于克服皮肤的屏障特性和活性剂的光降解。在本研究中，壳聚糖还原的金纳米粒子被研究作为载体，通过喷雾干燥法制备脂质体。对所得脂质体进行了磷脂回收、漫反射红外傅里叶变换（DRIFT）光谱、粒径、Zeta 电位、包封效率以及药物和金纳米粒子在大鼠皮肤中的沉积的表征。此外，使用 Carbopol®980NF（Noveon Systems，印度科奇）制备了脂质体凝胶制剂，并评估了其在皮肤中的药物沉积。在人白血病（HL-60）细胞系上测定了包封在金脂质体中的维生素 C 的抗氧化活性。金纳米粒子作为载体的使用显示出改善的磷脂回收，从而克服了脂质体的可扩展性问题。DRIFT 光谱证实了制剂中存在磷脂。与对照和市售制剂相比，脂质体凝胶显示出改善的药物沉积。壳聚糖还原的金纳米粒子的一个更有趣的贡献是，在负载维生素 C 的金脂质体制剂中观察到增强的抗氧化活性。脂质体制剂在 30°C 和 65%相对湿度下稳定 3 个月。
