The aim of this study was to improve the transdermal permeation of Diclofenac sodium, a poorly water-soluble drug, employing conventional liposomes, ethosomes, and transfersomes. The prepared formulations had been characterized for the loaded drug amount and vesicle size. The prepared vesicular systems were incorporated into 1% Carbopol 914 gel, and a survey of in vitro drug release and drug retention into rat skin has been done on them using a modified Franz diffusion cell. The cumulative amount of drug permeated after 24 h, flux, and permeability coefficient were assessed. Stability studies were performed for three months. The size of vesicles ranged from 145 to 202 nm, and the encapsulation efficiency of the Diclofenac sodium was obtained between 42.61% and 51.72%. The transfersomes and ethosomes provided a significantly higher amount of cumulative permeation, steady state flux, permeability coefficient, and residual drug into skin compared to the conventional liposomes, conventional gel, or hydroethanolic solution. The in vitro release data of all vesicular systems were well fit into Higuchi model (RSD > 0.99). Stability tests indicated that the vesicular formulations were stable over three months. Results revealed that both ethosome and transfersome formulations can act as drug reservoir in skin and extend the pharmacologic effects of Diclofenac sodium.
Cancer is considered as one of the most severe health problems and is currently the third most common cause of death in the world after heart and infectious diseases. Novel therapies are constantly being discovered, developed and trialed. Many of the current anticancer agents exhibit non-ideal pharmaceutical and pharmacological properties and are distributed non-specifically throughout the body. This results in death of the both normal healthy and malignant cells and substantially leads to accruing a variety of serious toxic side effects. Therefore, the efficient systemic therapy of cancer is almost impossible due to harmful side effects of anticancer agents to the healthy organs and tissues. Furthermore, several problems such as low bioavailability of the drugs, low drug concentrations at the site of action, lack of drug specificity and drug-resistance also cause many restrictions on clinical applications of these drugs in the tumor therapy. Different types of the liposomal formulations have been used in medicine due to their distinctive advantages associated with their structural flexibility in the encapsulation of various agents with different physicochemical properties. They can also mediate delivery of the cargo to the appropriate cell type and subcellular compartment, reducing the effective dosage and possible side effects which are related to high systemic concentrations. Therefore, these novel systems were found very promising and encouraging dosage forms for the treatment of different types of cancer by increasing efficiency and reducing the systemic toxicity due to the specific drug delivery and targeting.
Results indicated that essential oil of S. sclareoides includes rather higher proportions of non-terpenoid and sesquiterpenes compounds with good antioxidant and antibacterial properties.
Objective: The objective of this study was to formulate and evaluate the Ibuprofen niosomal formulation as a transdermal drug delivery system. Materials and methods: Niosomes were prepared by a modified ethanol injection method, using Span 60, Tween 60 and Tween 65 as well as cholesterol with various cholesterol:surfactant molar ratios. The prepared vesicles were characterized for entrapment efficiency (EE), particle size, zeta potential and in vitro release study. Skin permeation studies were conducted using modified Franz diffusion cell, and excised rat skin was treated with niosomal, liposomal and conventional Carbopol 914 gel of Ibuprofen. Results and discussion: The results showed that the type of surfactant and molar ratio of cholesterol:surfactant altered the EE, size and in vitro drug release of niosomes. Higher EE was obtained with the niosomes prepared with cholesterol and Span 60 at molar ratio of 0.5:1. It has been observed that both niosomal and liposomal formulations enhanced the drug permeation and the percentage of accumulated dose in the skin compared to control conventional gel formulation. However, niosomes prepared by Span 60 and Tween 65 exhibited higher permeation and retention of Ibuprofen, respectively. Conclusion: Our results suggested that niosomal formulations could be used as a promising carrier for the Ibuprofen transdermal delivery system.
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