Transdermal delivery of levonorgestrel

Friend, David R.

doi:10.1002/med.2610110105

Cited by 19 publications

(4 citation statements)

References 67 publications

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“…Ethylacetate, methylacetate, butylacetate and methylpropionate are used as well as isopropyl-n-butyrate, isopropyl-n-decanoate, isopropylmyristate and isopropylpalmitate for example. Ethyl acetate was found to be the best penetration enhancer for the transdermal delivery of the contraceptive levonorgestrel [77] . The ester was able to speed up absorption 17-fold in rat skin.…”

Section: Estersmentioning

confidence: 99%

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Trommer

Neubert

2006

Skin Pharmacol Physiol

460

279

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It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not have the ability to penetrate the stratum corneum. In these cases modulations of the skin penetration profiles of these drugs and skin barrier manipulations are necessary. A skin penetration enhancement can be achieved either chemically, physically or by use of appropriate formulations. Numerous chemical compounds have been evaluated for penetration-enhancing activity, and different modes of action have been identified for skin penetration enhancement. In addition to chemical methods, skin penetration of drugs can be improved by physical options such as iontophoresis and phonophoresis, as well as by combinations of both chemical and physical methods or by combinations of several physical methods. There are cases where skin penetration of the drug used in the formulation is not the aim of the topical administration. Penetration reducers can be used to prevent chemicals entering the systemic circulation. This article concentrates on the progress made mainly over the last decade by use of chemical penetration enhancers. The different action modes of these substances are explained, including the basic principles of the physical skin penetration enhancement techniques and examples for their application.

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Section: Estersmentioning

confidence: 99%

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Trommer

Neubert

2006

Skin Pharmacol Physiol

460

279

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“…Matrix patches are typically associated with fewer skin reactions than earlier reservoir patches due to improved air circulation and absence of alcohol-based solvents [50]. Studies on similarly designed TDDS delivering hormones have established low risk of skin irritation, pruritis, urticaria, and did not notice local effects of the medication [51][52][53]. Mild sub-acute irritation and erythema have been observed in patch formulations lacking drug as well, indicating that occlusion by the patch itself may contribute to skin irritation, while any local dermal effects by the drug were reversible [54].…”

Section: Discussionmentioning

confidence: 99%

Development and In Vitro Testing of a Novel Universal Transdermal Drug Delivery Platform to Reduce Medication Nonadherence

Ramesh¹,

Zamat²,

Vadlamudi³

et al. 2022

J Drug Res Dev

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Medication nonadherence results in avoidable symptom exacerbations and hospitalization, causing thousands of deaths and billions of dollars in healthcare costs annually. Although pharmacological therapies are present for chronic diseases, lengthy and complicated medication regimens often have high rates of nonadherence. Transdermal drug delivery is a potential method of reducing medication nonadherence as it allows for long-course medication regimens to be simplified to a one-time epidermal patch. We have engineered a transdermal drug delivery system on a customizable platform to longitudinally deliver a wide variety of soluble small-molecule drugs. As a proof of concept, we have chosen to administer long-course corticosteroids for chronic inflammatory disease via epidermal patch. A drug-in-adhesive matrix consisting of the drug, adhesive, solvents, and penetration enhancers, was cured onto a fluoropolymer release liner. The transdermal drug delivery system has an integrated tapering mechanism to avoid end-of-course steroid dependence and can incorporate other small-molecule medications required for cases of polypharmacy. To date, there have been no successful attempts to develop long-term steroid patches for systemic delivery, which may be attributed to issues with patch adhesion and skin irritation over extended periods of time. We have analyzed such challenges and have designed a proof of concept system to overcome these obstacles in order to provide patients with a simple, inexpensive, and effective solution to complicated and long-term treatment regimens.

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“…We were interested to note that EVA copolymers are used for transdermal drug delivery systems (4) as penetration enhancers (5), and questioned an EVA effect on absorption of rubber additives from these shoes. Correspondence with Crocs Inc. to ascertain which chemicals were used in the manufacture of the shoe and their interactions proved unsuccessful, as ‘proprietary status’ prevented the disclosure (Crocs Inc – Customer Service, personal communication, August 2007).…”

Section: Discussionmentioning

confidence: 99%