Abstract The present work is designed to achieve efficient localised skin delivery of folic acid ... more Abstract The present work is designed to achieve efficient localised skin delivery of folic acid (FA)–loaded nanostructured lipid carriers (NLCs) to infer efficient treatment of skin photoageing conditions induced via excessive exposure to ultraviolet (UV) radiation. FA NLCs were prepared by high-speed homogenisation followed by ultrasonication. The obtained NLCs revealed high encapsulation efficiencies (89.42–99.26%) with nanometric particle sizes (27.06–85.36 nm) of monodisperse distribution (PDI = 0.137–0.442), zeta potential values >|27| mV, pseudoplastic rheological behaviour, good spreadability (2.25–3.30 cm) and promoted occlusive properties throughout 48 h. Optimised NLC formulations appeared as sphere-shaped particles using transmission electron microscopy, showed improved photostability of FA and prolonged in vitro release profile best fitted to Higuchi diffusion model. Ex vivo permeation and deposition of FA, employing Wistar rat skins, depicted enhanced permeability and existence of FA in skin layers after 6 h. Based on the obtained results, FA-loaded NLC formulations demonstrate a promising modality for anti-photoageing therapy.
The present comparative study aims at studying the effect of several adjuvents on enhancing the s... more The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimiz...
Ageing is the progressive deterioration of physiological functions in organisms. Folic acid (FA) ... more Ageing is the progressive deterioration of physiological functions in organisms. Folic acid (FA) can be used as antiaging. The objective of this research is the feasibility of topical delivery of FA using nanostructured lipid carriers (NLCs) to offer sustained antioxidant and antiaging effects. FA NLCS were prepared by hot high pressure homogenization. Encapsulation efficiency (EE), in vitro release, ex vivo permeation and skin targeting were evaluated. Characterization of selected formulations was assessed, together with stability and water occlusion. Further, histology and antioxidant potential were evaluated. EE exceeded 95%. Formulations with 30% oil showed maximum skin targeting, water occlusion and high efficiency of hydration and antioxidant potential. Incorporation of oil into solid lipids causes more imperfections in the crystal lattice, providing high drug encapsulation. The small particle size leads to forming a depot in the skin providing efficient skin targeting, water occlusion, antiaging and antioxidant effects especially for the 30% oil containing formula; F11. The results emphasize the success of topical application of FA NLCs. F11 represents a promising, stable preparation, achieving remarkable long acting skin hydration, in vitro and ex vivo antioxidant potential lasting for >4 days.
The present comparative study aims at studying the effect of several adjuvents on enhancing the s... more The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimized selected formulation was successfully stable in refrigerator temperature throughout 9 months of the study. The TEM photograph reveals the formation of rounded nano vesicles. The present study was successful in development of more stable, more sustained means for topical delivery of FA for future cosmoceutical benefits.
Abstract The present work is designed to achieve efficient localised skin delivery of folic acid ... more Abstract The present work is designed to achieve efficient localised skin delivery of folic acid (FA)–loaded nanostructured lipid carriers (NLCs) to infer efficient treatment of skin photoageing conditions induced via excessive exposure to ultraviolet (UV) radiation. FA NLCs were prepared by high-speed homogenisation followed by ultrasonication. The obtained NLCs revealed high encapsulation efficiencies (89.42–99.26%) with nanometric particle sizes (27.06–85.36 nm) of monodisperse distribution (PDI = 0.137–0.442), zeta potential values >|27| mV, pseudoplastic rheological behaviour, good spreadability (2.25–3.30 cm) and promoted occlusive properties throughout 48 h. Optimised NLC formulations appeared as sphere-shaped particles using transmission electron microscopy, showed improved photostability of FA and prolonged in vitro release profile best fitted to Higuchi diffusion model. Ex vivo permeation and deposition of FA, employing Wistar rat skins, depicted enhanced permeability and existence of FA in skin layers after 6 h. Based on the obtained results, FA-loaded NLC formulations demonstrate a promising modality for anti-photoageing therapy.
The present comparative study aims at studying the effect of several adjuvents on enhancing the s... more The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimiz...
Ageing is the progressive deterioration of physiological functions in organisms. Folic acid (FA) ... more Ageing is the progressive deterioration of physiological functions in organisms. Folic acid (FA) can be used as antiaging. The objective of this research is the feasibility of topical delivery of FA using nanostructured lipid carriers (NLCs) to offer sustained antioxidant and antiaging effects. FA NLCS were prepared by hot high pressure homogenization. Encapsulation efficiency (EE), in vitro release, ex vivo permeation and skin targeting were evaluated. Characterization of selected formulations was assessed, together with stability and water occlusion. Further, histology and antioxidant potential were evaluated. EE exceeded 95%. Formulations with 30% oil showed maximum skin targeting, water occlusion and high efficiency of hydration and antioxidant potential. Incorporation of oil into solid lipids causes more imperfections in the crystal lattice, providing high drug encapsulation. The small particle size leads to forming a depot in the skin providing efficient skin targeting, water occlusion, antiaging and antioxidant effects especially for the 30% oil containing formula; F11. The results emphasize the success of topical application of FA NLCs. F11 represents a promising, stable preparation, achieving remarkable long acting skin hydration, in vitro and ex vivo antioxidant potential lasting for >4 days.
The present comparative study aims at studying the effect of several adjuvents on enhancing the s... more The present comparative study aims at studying the effect of several adjuvents on enhancing the stability and sustainability of FA NLCs which previously showed very promising results. The problem was encountered in the high drug release, high skin permeation, low deposition and low stability. In the present study, propylene glycol was added to all preparations as a stabilizer and coemulsifier. Plurol® stearique was utilized as solid lipid and stabilizer instead of apifil®. Soft paraffin was used as a softening additional lipid to Plurol® stearique to ensure the amorphous structure of NLCs. Liquid paraffin was used for its emollient effect instead of capryol ™ 90 with Apifil®. The in vitro drug release, ex vivo drug permeation and skin deposition were analyzed. Selection of the most optimum formulation is achieved to investigate its photostability, long term stability. Also, it was photographed under TEM. The selected formulation was stable after six hours of irradiation. The optimized selected formulation was successfully stable in refrigerator temperature throughout 9 months of the study. The TEM photograph reveals the formation of rounded nano vesicles. The present study was successful in development of more stable, more sustained means for topical delivery of FA for future cosmoceutical benefits.
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