Formulation considerations in the design of topical, polymeric film-forming systems for sustained drug delivery to the skin

Kit Frederiksen, Richard H. Guy, Karsten Petersson

Research output: Contribution to journalArticle

28 Citations (Scopus)
187 Downloads (Pure)

Abstract

Polymeric film-forming systems (FFSs) are potential drug delivery systems for topical application to the skin. The FFSs form thin and transparent polymeric films in situ upon solvent evaporation. Their application convenience and cosmetic attributes, superior to conventional semi-solids, may offer improved patient compliance. This study represents the first phase of an investigation into the use of FFSs for prolonged dermal drug delivery. FFS formulations were distinguished based on their ability to sustain the release of betamethasone 17-valerate (BMV) in vitro over 72 h. The effect of film-forming polymer (hydrophilic: hydroxypropyl cellulose (Klucel™ LF); hydrophobic: polymethacrylate copolymers (Eudragit® NE and Eudragit® RS), and polyacrylate copolymer (Dermacryl® 79) was first determined, and then the impact of incorporation of plasticisers (triethyl citrate, tributyl citrate, and dibutyl sebacate) was examined. The Klucel film released a significantly higher amount of BMV than the hydrophobic FFS, 42 versus 4 μg/cm2, respectively. The release was increased when a plasticiser was incorporated, and with higher enhancement ratios achieved with the more lipophilic plasticisers. In conclusion, the results show that FFSs can sustain drug release (hence representing useful systems for prolonged dermal therapy) and emphasise the importance of the formulation on drug delivery, with the type of polymer being of greatest significance.

Original languageEnglish
Pages (from-to)9-15
Number of pages7
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume91
Early online date13 Jan 2015
DOIs
Publication statusPublished - Apr 2015

Fingerprint

Plasticizers
Drug Delivery Systems
Betamethasone Valerate
Skin
Polymers
Drug Compounding
Aptitude
Patient Compliance
Cosmetics
Pharmaceutical Preparations
Therapeutics

Keywords

  • Betamethasone 17-valerate
  • In vitro release
  • Keywords Dermal drug delivery
  • Plasticiser
  • Polymeric film-forming systems
  • Sustained release

Cite this

@article{263632ef06b44b889f13ec963135d691,
title = "Formulation considerations in the design of topical, polymeric film-forming systems for sustained drug delivery to the skin",
abstract = "Polymeric film-forming systems (FFSs) are potential drug delivery systems for topical application to the skin. The FFSs form thin and transparent polymeric films in situ upon solvent evaporation. Their application convenience and cosmetic attributes, superior to conventional semi-solids, may offer improved patient compliance. This study represents the first phase of an investigation into the use of FFSs for prolonged dermal drug delivery. FFS formulations were distinguished based on their ability to sustain the release of betamethasone 17-valerate (BMV) in vitro over 72 h. The effect of film-forming polymer (hydrophilic: hydroxypropyl cellulose (Klucel™ LF); hydrophobic: polymethacrylate copolymers (Eudragit{\circledR} NE and Eudragit{\circledR} RS), and polyacrylate copolymer (Dermacryl{\circledR} 79) was first determined, and then the impact of incorporation of plasticisers (triethyl citrate, tributyl citrate, and dibutyl sebacate) was examined. The Klucel film released a significantly higher amount of BMV than the hydrophobic FFS, 42 versus 4 μg/cm2, respectively. The release was increased when a plasticiser was incorporated, and with higher enhancement ratios achieved with the more lipophilic plasticisers. In conclusion, the results show that FFSs can sustain drug release (hence representing useful systems for prolonged dermal therapy) and emphasise the importance of the formulation on drug delivery, with the type of polymer being of greatest significance.",
keywords = "Betamethasone 17-valerate, In vitro release, Keywords Dermal drug delivery, Plasticiser, Polymeric film-forming systems, Sustained release",
author = "Kit Frederiksen and Guy, {Richard H.} and Karsten Petersson",
year = "2015",
month = "4",
doi = "10.1016/j.ejpb.2015.01.002",
language = "English",
volume = "91",
pages = "9--15",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",

}

TY - JOUR

T1 - Formulation considerations in the design of topical, polymeric film-forming systems for sustained drug delivery to the skin

AU - Frederiksen, Kit

AU - Guy, Richard H.

AU - Petersson, Karsten

PY - 2015/4

Y1 - 2015/4

N2 - Polymeric film-forming systems (FFSs) are potential drug delivery systems for topical application to the skin. The FFSs form thin and transparent polymeric films in situ upon solvent evaporation. Their application convenience and cosmetic attributes, superior to conventional semi-solids, may offer improved patient compliance. This study represents the first phase of an investigation into the use of FFSs for prolonged dermal drug delivery. FFS formulations were distinguished based on their ability to sustain the release of betamethasone 17-valerate (BMV) in vitro over 72 h. The effect of film-forming polymer (hydrophilic: hydroxypropyl cellulose (Klucel™ LF); hydrophobic: polymethacrylate copolymers (Eudragit® NE and Eudragit® RS), and polyacrylate copolymer (Dermacryl® 79) was first determined, and then the impact of incorporation of plasticisers (triethyl citrate, tributyl citrate, and dibutyl sebacate) was examined. The Klucel film released a significantly higher amount of BMV than the hydrophobic FFS, 42 versus 4 μg/cm2, respectively. The release was increased when a plasticiser was incorporated, and with higher enhancement ratios achieved with the more lipophilic plasticisers. In conclusion, the results show that FFSs can sustain drug release (hence representing useful systems for prolonged dermal therapy) and emphasise the importance of the formulation on drug delivery, with the type of polymer being of greatest significance.

AB - Polymeric film-forming systems (FFSs) are potential drug delivery systems for topical application to the skin. The FFSs form thin and transparent polymeric films in situ upon solvent evaporation. Their application convenience and cosmetic attributes, superior to conventional semi-solids, may offer improved patient compliance. This study represents the first phase of an investigation into the use of FFSs for prolonged dermal drug delivery. FFS formulations were distinguished based on their ability to sustain the release of betamethasone 17-valerate (BMV) in vitro over 72 h. The effect of film-forming polymer (hydrophilic: hydroxypropyl cellulose (Klucel™ LF); hydrophobic: polymethacrylate copolymers (Eudragit® NE and Eudragit® RS), and polyacrylate copolymer (Dermacryl® 79) was first determined, and then the impact of incorporation of plasticisers (triethyl citrate, tributyl citrate, and dibutyl sebacate) was examined. The Klucel film released a significantly higher amount of BMV than the hydrophobic FFS, 42 versus 4 μg/cm2, respectively. The release was increased when a plasticiser was incorporated, and with higher enhancement ratios achieved with the more lipophilic plasticisers. In conclusion, the results show that FFSs can sustain drug release (hence representing useful systems for prolonged dermal therapy) and emphasise the importance of the formulation on drug delivery, with the type of polymer being of greatest significance.

KW - Betamethasone 17-valerate

KW - In vitro release

KW - Keywords Dermal drug delivery

KW - Plasticiser

KW - Polymeric film-forming systems

KW - Sustained release

UR - http://www.scopus.com/inward/record.url?scp=84922229389&partnerID=8YFLogxK

UR - http://dx.doi.org/10.1016/j.ejpb.2015.01.002

U2 - 10.1016/j.ejpb.2015.01.002

DO - 10.1016/j.ejpb.2015.01.002

M3 - Article

AN - SCOPUS:84922229389

VL - 91

SP - 9

EP - 15

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

ER -