Formulation Strategies for Modulating Skin Permeation

Davis, Annette; Gyurik, Robert J.; Hadgraft, Jonathan; Pellett, Mark; Walters, K.

doi:10.1201/9780824743239.ch6

Cited by 18 publications

(15 citation statements)

References 143 publications

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“…This had previously been reported for mixtures of Azone and propylene glycol (Wotton et al, 1985). Supersaturation was described above and it is also possible to obtain synergistic effects when supersaturation is combined with chemical penetration enhancement (Davis et al, 2002).…”

Section: Penetration Enhancersmentioning

confidence: 85%

Advanced topical formulations (ATF)

Hadgraft¹,

Lane²

2016

International Journal of Pharmaceutics

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Topical formulations aim to target the skin for a variety of cosmetic, protective or therapeutic needs. Despite the use of creams and ointments over the millennia, the bioavailability of actives from topical preparations remains quite low, often not exceeding 1-2% of the applied dose. In this review we examine the reasons underlying the poor performance of topical preparations. We also outline a rational approach, based on Fick's laws of diffusion, to develop advanced topical formulations. Methodologies which are currently used in research and development are critically examined and the importance of understanding the fate of the vehicle as well as the active is emphasised. Advanced topical formulation development will also be facilitated by emerging and sophisticated analytical techniques that are able to probe real time delivery of actives to the skin. A good understanding of the underlying physical chemistry of both the formulation and the skin is crucial in the development of optimised topical products.

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Section: Penetration Enhancersmentioning

confidence: 85%

Advanced topical formulations (ATF)

Hadgraft¹,

Lane²

2016

International Journal of Pharmaceutics

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“…Treatment of inflammatory skin diseases frequently requires a combination of systemic and topical agents, but topical substances alone are very often adequate (1)(2)(3)(4)(5).…”

Section: Introductionmentioning

confidence: 99%

Control of Transdermal Permeation of Hydrocortisone Acetate from Hydrophilic and Lipophilic Formulations

et al. 2008

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Abstract. The purpose of this research was the preparation of four formulations containing hydrocortisone acetate (HCA) for topical application, including two aqueous systems (hydrophilic microemulsion and aqueous gel) and two systems with dominant hydrophobicity (hydrophobic microemulsion and ointment). The formulations were tested for the release and permeation of HCA across an animal membrane. The release of HCA was found comparable for the four systems. The two microemulsions promote permeation across an ex-vivo membrane, examined by means of a Franz cell. Hydrophobic microemulsion guarantees the highest solubility (2,370 μg/ml) and flux (133 μg/cm 2 .h) of the drug, since it contains almost 40% Transcutol, a permeation enhancer. Gel and ointment provide lower solubility and flux, being the values, related to the ointment, the lowest ones (562 μg/ml and 0.4 μg/ cm 2 .h). Experimental results allow the conclusion that gel and ointment can be suitable when it is desirable to minimize absorption of topically applied HCA as to keep the drug restricted to the diseased area and prevent side effects of the systemic presence of HCA.

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“…In the last few years strategies have been developed in order to increase the efficacy of the vehicle [26]. They may be of chemical, biochemical or physical order.…”

Section: Methods Of Modulation Of Cutaneous Permeabilitymentioning

confidence: 99%