Topical Nano and Microemulsions for Skin Delivery

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Abstract

Nanosystems such as microemulsions (ME) and nanoemulsions (NE) offer considerable opportunities for targeted drug delivery to and via the skin. ME and NE are stable colloidal systems composed of oil and water, stabilised by a mixture of surfactants and cosurfactants, that have received particular interest as topical skin delivery systems. There is considerable scope to manipulate the formulation components and characteristics to achieve optimal bioavailability and minimal skin irritancy. This includes the incorporation of established chemical penetration enhancers to fluidize the stratum corneum lipid bilayers, thus reducing the primary skin barrier and increasing permeation. This review discusses nanosystems with utility in skin delivery and focuses on the composition and characterization of ME and NE for topical and transdermal delivery. The mechanism of skin delivery across the stratum corneum and via hair follicles is reviewed with particular focus on the influence of formulation.

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Nanoemulsions: formation, properties and applications.

Ankur Gupta, H Burak Eral, T. Alan Hatton … (2016)

Nanoemulsions are kinetically stable liquid-in-liquid dispersions with droplet sizes on the order of 100 nm. Their small size leads to useful properties such as high surface area per unit volume, robust stability, optically transparent appearance, and tunable rheology. Nanoemulsions are finding application in diverse areas such as drug delivery, food, cosmetics, pharmaceuticals, and material synthesis. Additionally, they serve as model systems to understand nanoscale colloidal dispersions. High and low energy methods are used to prepare nanoemulsions, including high pressure homogenization, ultrasonication, phase inversion temperature and emulsion inversion point, as well as recently developed approaches such as bubble bursting method. In this review article, we summarize the major methods to prepare nanoemulsions, theories to predict droplet size, physical conditions and chemical additives which affect droplet stability, and recent applications.

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Penetration enhancers.

Adrian C. Williams, Brian W. Barry (2004)

One long-standing approach for improving transdermal drug delivery uses penetration enhancers (also called sorption promoters or accelerants) which penetrate into skin to reversibly decrease the barrier resistance. Numerous compounds have been evaluated for penetration enhancing activity, including sulphoxides (such as dimethylsulphoxide, DMSO), Azones (e.g. laurocapram), pyrrolidones (for example 2-pyrrolidone, 2P), alcohols and alkanols (ethanol, or decanol), glycols (for example propylene glycol, PG, a common excipient in topically applied dosage forms), surfactants (also common in dosage forms) and terpenes. Many potential sites and modes of action have been identified for skin penetration enhancers; the intercellular lipid matrix in which the accelerants may disrupt the packing motif, the intracellular keratin domains or through increasing drug partitioning into the tissue by acting as a solvent for the permeant within the membrane. Further potential mechanisms of action, for example with the enhancers acting on desmosomal connections between corneocytes or altering metabolic activity within the skin, or exerting an influence on the thermodynamic activity/solubility of the drug in its vehicle are also feasible, and are also considered in this review.

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Design and production of nanoparticles formulated from nano-emulsion templates-a review.

Nicolas Anton, Jean-Pierre Benoit, Patrick Saulnier (2008)

A considerable number of nanoparticle formulation methods are based on nano-emulsion templates, which in turn are generated in various ways. It must therefore be taken into account that active principles and drugs encapsulated in nanoparticles can potentially be affected by these nano-emulsion formulation processes. Such potential differences may include drug sensitivity to temperature, high-shear devices, or even contact with organic solvents. Likewise, nano-emulsion formulation processes must be chosen in function of the selected therapeutic goals of the nano-carrier suspension and its administration route. This requires the nanoparticle formulation processes (and thus the nano-emulsion formation methods) to be more adapted to the nature of the encapsulated drugs, as well as to the chosen route of administration. Offering a comprehensive review, this paper proposes a link between nano-emulsion formulation methods and nanoparticle generation, while at the same time bearing in mind the above-mentioned parameters for active molecule encapsulation. The first part will deal with the nano-emulsion template through the different formulation methods, i.e. high energy methods on the one hand, and low-energy ones (essentially spontaneous emulsification and the phase inversion temperature (PIT) method) on the other. This will be followed by a review of the different families of nanoparticles (i.e. polymeric or lipid nanospheres and nanocapsules) highlighting the links (or potential links) between these nanoparticles and the different nano-emulsion formulation methods upon which they are based.

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Author and article information

Journal

Journal ID (nlm-ta): Pharmaceutics

Journal ID (iso-abbrev): Pharmaceutics

Journal ID (publisher-id): pharmaceutics

Title: Pharmaceutics

Publisher: MDPI

ISSN (Electronic): 1999-4923

Publication date (Electronic): 21 September 2017

Publication date Collection: December 2017

Volume: 9

Issue: 4

Electronic Location Identifier: 37

Affiliations

[1 ]School of Pharmacy, Curtin Health Innovation Research Institute, Curtin University, G.P.O. Box U1987, Perth, WA 6845, Australia; c.nastiti@ 123456postgrad.curtin.edu.au (C.M.R.R.N.); thellie.ponto@ 123456postgrad.curtin.edu.au (T.P.); H.Benson@ 123456curtin.edu.au (H.A.E.B.)

[2 ]Faculty of Pharmacy, Sanata Dharma University, Yogyakarta 55282, Indonesia

[3 ]Therapeutics Research Centre, The University of Queensland Diamentina Institute, Faculty of Medicine, Translational Research Institute, Woolloongabba, QLD 4102, Australia; e.abd@ 123456uq.edu.au (E.A.); jeff.grice@ 123456uq.edu.au (J.E.G.)

[4 ]School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA 5000, Australia

Author notes

[* ]Correspondence: m.roberts@ 123456uq.edu.au ; Tel.: +61-7-34438031; Fax: +61-7-34437779

[†]

These authors contributed equally to this work.

Article

Publisher ID: pharmaceutics-09-00037

DOI: 10.3390/pharmaceutics9040037

PMC ID: 5750643

PubMed ID: 28934172

SO-VID: e9ec6a7e-00bc-4e90-a66a-f8f405790045

License:

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

Topical Nano and Microemulsions for Skin Delivery

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Abstract

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RNA drug delivery

Most cited references 95

Nanoemulsions: formation, properties and applications.

Penetration enhancers.

Design and production of nanoparticles formulated from nano-emulsion templates-a review.

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