فرمولاسیون و ارزیابی لیپوزوم موضعی دوکسپین در درمان اگزمای پوستی

عنوان انگليسی

Formulation and Evaluation of Topical Liposomal Doxepin for Treatment of Eczema

خلاصه انگلیسی

Introduction Liposomal drug delivery is one of the novel methods for improving topical/transdermal drug delivery. Topical liposomes are preferred due to advantages such as high capacity for drug loading and the ability to deliver it to the epidermis and deeper layers of skin. Moreover, fewer side effects, shorter treatment lengths and better effect are other advantages of liposomes. Topical liposomes by their sustained released effect can increase the concentration of drug in the deeper layers of the skin. Doxepin, a tricyclic antidepressant agent is a potent antagonist for H1,H2 and muscarinic receptors. On the other hand, doxepin has anti-pruritic effects. Oral administration of this drug leads to the hypnotic effects and anti-cholinergic complications such as blurred vision, dry mouth, urinary retention, etc. Oral doxepin is used to treat chronic and acute eczema, but the systemic adverse effects can reduce its efficacy. For this purpose, its topical cream is used to reduce itching, which has a slight absorption to blood compared with oral form. Liposomal formulation of doxepin was studied to increase remaining in the skin layers and to reduce systemic absorption and consequently side effects. Methods In this study, the topical liposomal formulation of doxepin was prepared using thin film hydration method. At this stage, we use cholesterol and lecithin phospholipids to prepare the appropriate liposome for the drug. The obtained liposomes are evaluated in terms of properties such as size, zeta potential, shape and loading efficiency of the drug by using SEM, DLS and HPLC. For skin permeability assessment, the skin was extracted from laboratory mice and mounted on a Franz diffusion cell to evaluate the permeability of the prepared liposome and analyze the samples. Results The images from the light and electron microscope are shown below. The shape of the liposomes is spherical and the size is below 100 nm. Loading efficiency measured by HPLC (The mobile phase include deionized water, acetonitrile and methanol at 220 nm) was 46%.

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