Promotion of cutaneous penetration of nifedipine for nanoemulsion

Paula De Oliveira Arantes,Elisabete Pereira Dos Santos,Quesia Nery Dos Santos,Eduardo Ricci-Júnior,Ana Lucia Vazquez Villa,Cristal Cerqueira-Coutinho,Alexandre Dos Santos Pyrrho,Zaida Maria Faria De Freitas

doi:10.1590/s2175-97902017000215249

Paula De Oliveira Arantes, Elisabete Pereira Dos Santos + Show 6 more

Open Access

https://doi.org/10.1590/s2175-97902017000215249

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Abstract

ABSTRACT This article reports the development and characterization of a nanoemulsion (NE) able to improve the cutaneous penetration of nifedipine. NE with nifedipine was development and characterized, presenting droplet size of 20 nm with low polydispersity index (IP<0.1), spherical shape without aggregation, pH compatible with typical skin levels and stability evaluated by seven months. In the permeation studies, a classical formulation based in an oil/water cream containing nifedipine was used for comparison with NE. Nanoemulsion promoted and improved the retention of nifedipine in the epidermis and dermis in relation to classical formulation. This promoting effect is related to the nanometric size of the droplets of the NE (20 nm), which give him a large superficial area, favoring the contact of the nanocarrier with the skin surface. The NE was efficient in promoting accumulation of nifedipine in the dermis, which is the site of vasodilation action. NE was not irritating according to the primary dermal irritation tests. NE is a promising release system to promote cutaneous penetration of nifedipine and can be used in the future in clinical trials to promote healing of lesions caused by peripheral vascular diseases.

Highlights

Topical nifedipine is used for various purposes, such as treatment of periocular and face wrinkles (Innocenti et al, 2010; Calabro et al, 2014), closure of anal fissures (Golfam et al, 2010; Katsinelos et al, 2006), and to promote healing of skin wounds (Smith 2010; Melo et al, 2008; Ebadi et al, 2003)
Nifedipine was purchased from Pharmanostra (Brazil); Tween 20® was acquired from Tédia (Brazil); Pluronic F127® was purchased from Sigma Aldrich (USA); peppermint essential oil was acquired from Ferquima (Brazil); and Transcutol P® was purchased from Brasquim (Brazil)
The 10% w/w proportion was the maximum oil phase amount that could be incorporated in the aqueous phase without impairing the nanoemulsions’ stability, because higher proportions caused an increase in the droplet diameter and polydispersity index

Summary

Introduction

Topical nifedipine is used for various purposes, such as treatment of periocular and face wrinkles (Innocenti et al, 2010; Calabro et al, 2014), closure of anal fissures (Golfam et al, 2010; Katsinelos et al, 2006), and to promote healing of skin wounds (Smith 2010; Melo et al, 2008; Ebadi et al, 2003). One of the main functions of the skin is to protect the organism from dehydration and harm from the environment. It is formed by the epidermis, dermis and hypodermis. The top part of the epidermis is the stratum corneum (SC), composed of unviable keratinized cells called corneocytes. These cells are surrounded by a lipid bilayer and joined by a complex lipid matrix. Drugs formulations for topical use must have high penetration in the SC, bioaccumulation in the viable epidermis and dermis and low or no systemic absorption, to avoid adverse side effects.

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