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Encapsulation and Characterization of Nanoemulsions Based on an Anti-oxidative Polymeric Amphiphile for Topical Apigenin Delivery.

ABSTRACT: Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials. Nevertheless, its poor water solubility and low storage stability have limited its application feasibility on the pharmaceutical field. To address this issue, this study developed nanoemulsions (NEs) using an anti-oxidative polymeric amphiphile, d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydrogenated soy lecithin (HL), black soldier fly larvae (BSFL) oil, and avocado (AV) oil through pre-homogenization and ultrasonication method. Addition of TPGS (weight ratios 100 and 50% as compared to HL) into NEs effectively reduced particle size and phase transition region area of NEs with pure HL. Incorporation of Apig into NEs made particle size increase and provided a disorder effect on intraparticle molecular packing. Nevertheless, the encapsulation efficiency of NEs for Apig approached to about 99%. The chemical stability of Apig was significantly improved and its antioxidant ability was elevated by incorporation with BSFL oil and AV oil NEs, especially for NEs with single TPGS. NEs with single TPGS also exhibited the best Apig skin deposition. For future application of topical Apig delivery, NEs-gel was formed by the addition of hyaluronic acid (HA) into NEs. Their rheological characteristics were dominated by the surfactant ratios of HL to TPGS.

SUBMITTER: Chou TH

PROVIDER: S-EPMC8037426 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Herpetic infections caused by Herpes simplex virus (HSV) are among the most common human infections, affecting more than two quarters of the world's population. The standard treatment for orofacial herpes is the administration of antiviral drugs, mainly acyclovir (ACV). However, current products are mostly based on semisolid formulations that have limited ability to promote drug skin penetration and tend to leak from the application site, thus showing reduced ability to sustain local drug residence. This work reports on the production of poly (ε-caprolactone) (PCL) fibrous matrices with ACV and omega-3 fatty acids (ω3) for application as dressings to the topical treatment of orofacial herpes. PCL fibrous matrices with the co-incorporated bioactive compounds were obtained by electrospinning and characterized regarding their morphology, chemical, physical, and mechanical properties. The potential use of the developed polymeric fibrous matrices for topical applications was evaluated by: (i) the release kinetics of the bioactive compounds; (ii) the occlusive factor of the fibrous mat; (iii) ACV skin permeation capacity; and (iv) the cytotoxicity in a keratinocyte cell line. PCL fibrous matrices loaded with the bioactive compounds presented a smooth morphology and a good balance between flexibility and hardness essential to be durable for handling, while having a desirable texture to be used comfortably. The fibrous mat also provided a sustained release of ACV during 96 h and improved the skin permeability of this drug (Kp = 0.00928 ± 0.000867 cm/h) presenting also high porosity (74%) and a water vapor transmission rate (WVTR) of 881 ± 91 g/m2day, essential to maintain moist and oxygen for faster healing of herpes lesions. Furthermore, cytotoxicity studies suggest that the fibrous mat are safe for topical application. Overall, the PCL based electrospun fibrous matrices with ACV and ω3 hereby described have the potential to be used as therapeutic bandage systems for the treatment of orofacial herpes.

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Encapsulation and Characterization of Nanoemulsions Based on an Anti-oxidative Polymeric Amphiphile for Topical Apigenin Delivery.

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