Abstract
Objective: The flavonoidal drug Naringenin offers a natural defense against free radical generation due to their antioxidant i.e. free radical scavenging property. The continuation of research work towards the invention of targeting the flavonoidal drug for skin carcinoma. Naringenin is a potent antioxidant, having remarkable reactive oxygen species scavenging potential and abundantly found in citrus fruits.
 Methods: The optimization of the formulated mannosylated naringenin-loaded transfersomes (MA-NgTfs) was performed using Box–Behnken statistical design to obtain crucial variable parameters that influence vesicular size, size distribution and surface charge. Therefore keeping both the concepts in mind our objective is to design and optimize the mannosylated naringenin loaded transfersomes (MA-NgTfs) for macropahge targeting. The Box Behnken with 3D surface response design graph was employed to optimize the formulation.
 Results: Phospholipids and surfactant ratio played a remarkable role to determine the mean vesicular size and the Zeta potential of the vesicles. The Zeta potential is found in the formulation having a range of-18.01±1.05 to-28.7±1.008 mV represents the good stability of the formulation. The vesicles size range was found in the range of 102.4±1.01 to 263.74±0.63 and range of Entrapment efficiency of nanovesicles was as 72.04±1.53 to 82.04±0.81. In vitro drug release study shows that mannosylated naringenin loaded transfersomes (MA-NgTfs), and marketed formulation dispersion was found 69.31 %, 62.03 %, 58.71 %, and 65.02 % respectively. Ex vivo skin permeation and deposition study shows that the marketed product and pure drug suspension optimized transfersomes through the skin of mice was of flux 6.5±3.07 and the percentage of drug retention was 0.76±1.26. The results gave us strong evidence of cellular uptake bymannose–directed transfersomes via mannose receptor-based endocytosis.
 Conclusion: On the basis of findings, the study revealed that the prepared formulation has characteristic potential for targeting and the concept of ligand directed nanocarrier formulation was imparts synergistic effect against UV-induced skin carcinoma.
Highlights
Human skin is the largest organ and is highly exposed to environmental solar radiation and due to chronic long term exposure skin produces abnormal cell growth, which is responsible for the progression of skin cancer [1]
We proposed the macrophage targeting for skin cancer which may be useful for future perspective and effectively used as a site-specific drug delivery of Naringenin to the cancerous cells and decrease the adverse effect related to the drug and treat skin carcinoma synergistically [7]
The total lipid content and Tween 80 was mixed in a small amount of chloroform the plant active naringenin is about 20 mg and 10 mg of Dmannosamine HCl was dissolved in ethanol and the whole solution was subsequently added into lipid and Tween-80 mixture solution the solvent was evaporated at rotary evaporator (Buchi rota vapor R-3000 with 14000 water bath, Switzerland) until a dry layer of a mixture solution is formed and hydrated with phosphate buffer pH (5.5) at the temperature of 45 oC by rotation speed of 70 rpm and the nanovesicles forms were allowed to absorb and swell at room temperature for 3 hr
Summary
Human skin is the largest organ and is highly exposed to environmental solar radiation and due to chronic long term exposure skin produces abnormal cell growth, which is responsible for the progression of skin cancer [1]. The major objective of the skin cancer therapy is to develop such type of targeted drug delivery system that can able to deliver the medicaments at the site of action. We proposed the macrophage targeting for skin cancer which may be useful for future perspective and effectively used as a site-specific drug delivery of Naringenin to the cancerous cells and decrease the adverse effect related to the drug and treat skin carcinoma synergistically [7]. On the basis of previous findings, a formulation based on targeted therapy of natural bioactive for skin cancer is yet present in the market; our objective of the study was to conceptualize and formulate the optimized mannosylated naringenin loaded transfersomes based formulation for targeting macrophages of cancerous cells via Mannose ligand
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