In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions

Megan N Kelchen; Nicole K Brogden

doi:10.1007/s11095-018-2495-1

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In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions

Journal article

Peer reviewed

In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions

Megan N Kelchen and Nicole K Brogden

Pharmaceutical research, Vol.35(12), pp.228-12

10/09/2018

DOI: 10.1007/s11095-018-2495-1

PMCID: PMC6636348

PMID: 30302631

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Abstract

Topical beta-blockers are efficacious for treating infantile hemangiomas, but no formulations have been specifically optimized for skin delivery. Our objective was to quantify skin concentrations and drug permeation of propranolol (a nonselective beta-blocker) after application of microemulsions to intact and microneedle pretreated skin. Four propranolol-loaded microemulsions were characterized for droplet size, surface charge, conductivity, pH, drug solubility, and drug release. Skin concentrations and drug permeation through skin were quantified using LC-MS. Skin-to-receiver ratios were used to compare the microemulsion formulations to a drug-in-PBS solution. Propranolol solubility was significantly greater in microemulsions vs PBS. Cumulative drug release from the microemulsions over 24 h ranged from 13 to 26%. Skin concentrations and drug permeation through intact skin was significantly higher from PBS; however, the skin-to-receiver ratios were significantly higher for water-rich microemulsions compared to PBS or surfactant-rich microemulsions. Microneedle pretreatment significantly increased skin concentrations for all formulations. Skin-to-receiver ratios significantly increased after microneedle pretreatment for surfactant-rich microemulsions. Microemulsion formulation can be altered to elicit different drug delivery profiles through MN-treated skin. This could be advantageous for maximizing local skin drug concentrations and improving dosing schedules for infantile hemangioma treatment.

Administration, Cutaneous

Adrenergic beta-Antagonists - administration & dosage

Adrenergic beta-Antagonists - pharmacokinetics

Animals

Antihypertensive Agents - administration & dosage

Antihypertensive Agents - pharmacokinetics

Drug Carriers - chemistry

Drug Delivery Systems

Drug Liberation

Emulsions - chemistry

Hydrogen-Ion Concentration

Needles

Particle Size

Propranolol - administration & dosage

Propranolol - pharmacokinetics

Skin - metabolism

Skin Absorption

Solubility

Static Electricity

Swine

Details

Title: Subtitle: In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions
Creators: Megan N Kelchen - University of Iowa
Nicole K Brogden - University of Iowa
Resource Type: Journal article
Publication Details: Pharmaceutical research, Vol.35(12), pp.228-12
DOI: 10.1007/s11095-018-2495-1
PMID: 30302631
PMCID: PMC6636348
ISSN: 0724-8741
eISSN: 1573-904X
Grant note: R35GM124551 / National Institute of General Medical Sciences R35 GM124551 / NIGMS NIH HHS
Language: English
Date published: 10/09/2018
Academic Unit: Dermatology; Pharmaceutical Sciences and Experimental Therapeutics
Record Identifier: 9984296309902771

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30 Times Cited - Web of Science

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