Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation

Luteolin is a natural drug used as an antioxidant and anti-inflammatory, but unfortunately, it possesses low water solubility, which hinders its delivery via the skin. The main objective of this study was to prepare a luteolin-loaded nanosuspension by the antisolvent precipitation/sonication techniq...

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Autores principales:	Mohammed Elmowafy, Khaled Shalaby, Mohammad M. Al-Sanea, Omnia M. Hendawy, Ayman Salama, Mohamed F. Ibrahim, Mohammed M. Ghoneim
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	luteolin stabilizers nanosuspension skin delivery Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/3c09a3084cbf451d860e5092e43dcff1
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spelling	oai:doaj.org-article:3c09a3084cbf451d860e5092e43dcff12021-11-25T18:40:52ZInfluence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation10.3390/pharmaceutics131118121999-4923https://doaj.org/article/3c09a3084cbf451d860e5092e43dcff12021-10-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1812https://doaj.org/toc/1999-4923Luteolin is a natural drug used as an antioxidant and anti-inflammatory, but unfortunately, it possesses low water solubility, which hinders its delivery via the skin. The main objective of this study was to prepare a luteolin-loaded nanosuspension by the antisolvent precipitation/sonication technique and study the effects of four stabilizers (two nonionic stabilizers, Pluronic F127 and Tween 80, and two polymeric stabilizers, HPMC and alginate) on the physicochemical properties of the prepared formulations. The selected formulations were incorporated into a gel base to evaluate their skin permeability and anti-inflammatory efficacy. The particle size was in the nanosize range (in the range from 468.1 ± 18.6 nm to 1024.8 ± 15.9 nm), while the zeta potential was negative and in the range from −41.7 ± 6.3 mV to −15.3 ± 1.9 mV. In particular, alginate-stabilized nanosuspensions showed the smallest particle size, the highest zeta potential value, and excellent stability due to the dual stabilizing effects (electrostatic and steric effects). The DSC results revealed a less crystalline structure of luteolin in lyophilized NS2 and NS12. Formulations stabilized by 1% Pluronic (NS2) and 2% alginate (NS12) were incorporated into a carbopol 940 gel base and showed good organoleptic character (homogenous with no evidenced phase separation or grittiness). In vitro dissolution studies showed that NS12 enhanced luteolin release rates, indicating the effect of particle size on the drug release pattern. On the other hand, NS2 showed enhanced skin permeability and anti-inflammatory effect in a carrageenan-induced paw edema model, revealing the surface activity role of the stabilizers. In conclusion, while alginate increased the nanosuspension stability by means of dual stabilizing effects, Pluronic F127 improved the skin delivery and pharmacodynamic efficacy of luteolin.Mohammed ElmowafyKhaled ShalabyMohammad M. Al-SaneaOmnia M. HendawyAyman SalamaMohamed F. IbrahimMohammed M. GhoneimMDPI AGarticleluteolinstabilizersnanosuspensionskin deliveryPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1812, p 1812 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	luteolin stabilizers nanosuspension skin delivery Pharmacy and materia medica RS1-441
spellingShingle	luteolin stabilizers nanosuspension skin delivery Pharmacy and materia medica RS1-441 Mohammed Elmowafy Khaled Shalaby Mohammad M. Al-Sanea Omnia M. Hendawy Ayman Salama Mohamed F. Ibrahim Mohammed M. Ghoneim Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
description	Luteolin is a natural drug used as an antioxidant and anti-inflammatory, but unfortunately, it possesses low water solubility, which hinders its delivery via the skin. The main objective of this study was to prepare a luteolin-loaded nanosuspension by the antisolvent precipitation/sonication technique and study the effects of four stabilizers (two nonionic stabilizers, Pluronic F127 and Tween 80, and two polymeric stabilizers, HPMC and alginate) on the physicochemical properties of the prepared formulations. The selected formulations were incorporated into a gel base to evaluate their skin permeability and anti-inflammatory efficacy. The particle size was in the nanosize range (in the range from 468.1 ± 18.6 nm to 1024.8 ± 15.9 nm), while the zeta potential was negative and in the range from −41.7 ± 6.3 mV to −15.3 ± 1.9 mV. In particular, alginate-stabilized nanosuspensions showed the smallest particle size, the highest zeta potential value, and excellent stability due to the dual stabilizing effects (electrostatic and steric effects). The DSC results revealed a less crystalline structure of luteolin in lyophilized NS2 and NS12. Formulations stabilized by 1% Pluronic (NS2) and 2% alginate (NS12) were incorporated into a carbopol 940 gel base and showed good organoleptic character (homogenous with no evidenced phase separation or grittiness). In vitro dissolution studies showed that NS12 enhanced luteolin release rates, indicating the effect of particle size on the drug release pattern. On the other hand, NS2 showed enhanced skin permeability and anti-inflammatory effect in a carrageenan-induced paw edema model, revealing the surface activity role of the stabilizers. In conclusion, while alginate increased the nanosuspension stability by means of dual stabilizing effects, Pluronic F127 improved the skin delivery and pharmacodynamic efficacy of luteolin.
format	article
author	Mohammed Elmowafy Khaled Shalaby Mohammad M. Al-Sanea Omnia M. Hendawy Ayman Salama Mohamed F. Ibrahim Mohammed M. Ghoneim
author_facet	Mohammed Elmowafy Khaled Shalaby Mohammad M. Al-Sanea Omnia M. Hendawy Ayman Salama Mohamed F. Ibrahim Mohammed M. Ghoneim
author_sort	Mohammed Elmowafy
title	Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
title_short	Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
title_full	Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
title_fullStr	Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
title_full_unstemmed	Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation
title_sort	influence of stabilizer on the development of luteolin nanosuspension for cutaneous delivery: an in vitro and in vivo evaluation
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/3c09a3084cbf451d860e5092e43dcff1
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Influence of Stabilizer on the Development of Luteolin Nanosuspension for Cutaneous Delivery: An In Vitro and In Vivo Evaluation

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