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Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance

Authorized Users Only
2014
Authors
Pantelić, Ivana
Lukić, Milica
Marković, Bojan
Lusiana
Hoffmann, Christine
Mueller-Goymann, Christel
Milić, Jela
Daniels, Rolf
Savić, Snežana
Article (Published version)
Metadata
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Abstract
Context: Approaching of pharmaceutical and cosmetic industries in some aspects inevitably influence formulation of topical pharmaceuticals, urging researchers to introduce novel excipients with proven benefits over traditional ones. In that context, alkyl polyglucosides (APG) emerge as prominent natural-origin emulsifiers with numerous favorable features (biodegradability, dermatological acceptability, desirable sensory properties). Objective: To evaluate APG-stabilized bases (alone and upon addition of isopropyl alcohol) and their impact on skin performance. A simultaneous in vitro/in vivo skin absorption study was conducted to evaluate whether the tape stripping technique could be recommended as an in vivo tool for skin penetration assessment during formulation optimization process. Materials and methods: After a comprehensive physicochemical characterization, biopharmaceutical properties of APG-bases versus reference ones were assessed through a combined in vitro (release/permeation...) and in vivo approach. Results and discussion: Physicochemical characterization revealed substantial difference in structural ordering due to the formation of various mesomorphic phases. The enhancer-loaded APG base resulted in significantly higher drug levels at all depths into the stratum corneum, indicating that the selected enhancer along with specific colloidal structure has increased the extent of drug delivery. Conclusion: Results recommend the investigated emulsifier for stabilization of topical drug delivery systems, not only for their ability to sustain the addition of isopropyl alcohol which proved to be a valuable enhancer, but also satisfactory skin absorption and tolerability when compared to samples stabilized by conventional emulsifier. Tape stripping proved to be a useful and yet inexpensive tool for in vivo trials, able to discriminate subtle differences in dermal availability.

Keywords:
Alkyl polyglucosides / artificial skin constructs / Franz diffusion cells / isolated stratum corneum / tape stripping
Source:
Drug Development and Industrial Pharmacy, 2014, 40, 7, 960-971
Publisher:
  • Informa Healthcare, London
Projects:
  • Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)

DOI: 10.3109/03639045.2013.794827

ISSN: 0363-9045

PubMed: 23688275

WoS: 000337085500015

Scopus: 2-s2.0-84902279125
[ Google Scholar ]
7
6
URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/2194
Collections
  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy
TY  - JOUR
AU  - Pantelić, Ivana
AU  - Lukić, Milica
AU  - Marković, Bojan
AU  - Lusiana
AU  - Hoffmann, Christine
AU  - Mueller-Goymann, Christel
AU  - Milić, Jela
AU  - Daniels, Rolf
AU  - Savić, Snežana
PY  - 2014
UR  - http://farfar.pharmacy.bg.ac.rs/handle/123456789/2194
AB  - Context: Approaching of pharmaceutical and cosmetic industries in some aspects inevitably influence formulation of topical pharmaceuticals, urging researchers to introduce novel excipients with proven benefits over traditional ones. In that context, alkyl polyglucosides (APG) emerge as prominent natural-origin emulsifiers with numerous favorable features (biodegradability, dermatological acceptability, desirable sensory properties). Objective: To evaluate APG-stabilized bases (alone and upon addition of isopropyl alcohol) and their impact on skin performance. A simultaneous in vitro/in vivo skin absorption study was conducted to evaluate whether the tape stripping technique could be recommended as an in vivo tool for skin penetration assessment during formulation optimization process. Materials and methods: After a comprehensive physicochemical characterization, biopharmaceutical properties of APG-bases versus reference ones were assessed through a combined in vitro (release/permeation) and in vivo approach. Results and discussion: Physicochemical characterization revealed substantial difference in structural ordering due to the formation of various mesomorphic phases. The enhancer-loaded APG base resulted in significantly higher drug levels at all depths into the stratum corneum, indicating that the selected enhancer along with specific colloidal structure has increased the extent of drug delivery. Conclusion: Results recommend the investigated emulsifier for stabilization of topical drug delivery systems, not only for their ability to sustain the addition of isopropyl alcohol which proved to be a valuable enhancer, but also satisfactory skin absorption and tolerability when compared to samples stabilized by conventional emulsifier. Tape stripping proved to be a useful and yet inexpensive tool for in vivo trials, able to discriminate subtle differences in dermal availability.
PB  - Informa Healthcare, London
T2  - Drug Development and Industrial Pharmacy
T1  - Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance
VL  - 40
IS  - 7
SP  - 960
EP  - 971
DO  - 10.3109/03639045.2013.794827
ER  - 
@article{
author = "Pantelić, Ivana and Lukić, Milica and Marković, Bojan and Lusiana and Hoffmann, Christine and Mueller-Goymann, Christel and Milić, Jela and Daniels, Rolf and Savić, Snežana",
year = "2014",
url = "http://farfar.pharmacy.bg.ac.rs/handle/123456789/2194",
abstract = "Context: Approaching of pharmaceutical and cosmetic industries in some aspects inevitably influence formulation of topical pharmaceuticals, urging researchers to introduce novel excipients with proven benefits over traditional ones. In that context, alkyl polyglucosides (APG) emerge as prominent natural-origin emulsifiers with numerous favorable features (biodegradability, dermatological acceptability, desirable sensory properties). Objective: To evaluate APG-stabilized bases (alone and upon addition of isopropyl alcohol) and their impact on skin performance. A simultaneous in vitro/in vivo skin absorption study was conducted to evaluate whether the tape stripping technique could be recommended as an in vivo tool for skin penetration assessment during formulation optimization process. Materials and methods: After a comprehensive physicochemical characterization, biopharmaceutical properties of APG-bases versus reference ones were assessed through a combined in vitro (release/permeation) and in vivo approach. Results and discussion: Physicochemical characterization revealed substantial difference in structural ordering due to the formation of various mesomorphic phases. The enhancer-loaded APG base resulted in significantly higher drug levels at all depths into the stratum corneum, indicating that the selected enhancer along with specific colloidal structure has increased the extent of drug delivery. Conclusion: Results recommend the investigated emulsifier for stabilization of topical drug delivery systems, not only for their ability to sustain the addition of isopropyl alcohol which proved to be a valuable enhancer, but also satisfactory skin absorption and tolerability when compared to samples stabilized by conventional emulsifier. Tape stripping proved to be a useful and yet inexpensive tool for in vivo trials, able to discriminate subtle differences in dermal availability.",
publisher = "Informa Healthcare, London",
journal = "Drug Development and Industrial Pharmacy",
title = "Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance",
volume = "40",
number = "7",
pages = "960-971",
doi = "10.3109/03639045.2013.794827"
}
Pantelić I, Lukić M, Marković B, Lusiana, Hoffmann C, Mueller-Goymann C, Milić J, Daniels R, Savić S. Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance. Drug Development and Industrial Pharmacy. 2014;40(7):960-971
Pantelić, I., Lukić, M., Marković, B., Lusiana, Hoffmann, C., Mueller-Goymann, C., Milić, J., Daniels, R.,& Savić, S. (2014). Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance.
Drug Development and Industrial PharmacyInforma Healthcare, London., 40(7), 960-971.
https://doi.org/10.3109/03639045.2013.794827
Pantelić Ivana, Lukić Milica, Marković Bojan, Lusiana, Hoffmann Christine, Mueller-Goymann Christel, Milić Jela, Daniels Rolf, Savić Snežana, "Development of a prospective isopropyl alcohol-loaded pharmaceutical base using simultaneous in vitro/in vivo characterization methods of skin performance" 40, no. 7 (2014):960-971,
https://doi.org/10.3109/03639045.2013.794827 .

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