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Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form

Authorized Users Only
2019
Authors
Bubić Pajić, Nataša
Ilić, Tanja
Nikolić, Ines
Dobričić, Vladimir
Pantelić, Ivana
Savić, Snežana
Article (Published version)
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Abstract
Aiming to develop biocompatible microemulsions based on natural alkyl polyglucoside surfactant as prospective carriers for improved dermal delivery of adapalene, phase behavior and microstructure of pseudo-ternary oil/decyl glucoside/propylene glycol/water systems were evaluated. The chosen inverted bicontinuous formulations did not change their microstructure upon drug incorporation and remained stable during 1-year period. Preliminary in vivo assessment of skin performances suggested satisfying safety profiles of placebo microemulsions, in spite of considerable changes in skin hydration and barrier function. Interestingly, despite lower in vitro drug release, the amount of adapalene penetrated into porcine skin under infinite dosing regime was higher from microemulsions than from commercial drug product, reaching dermal retention enhancement ratio of 5.9. However, by changing experimental conditions to the more realistic in-use situation, the amount of adapalene extracted from the st...ratum corneum was comparable for microemulsions and marketed product. Similarly, the drug deposition in hair follicles was slightly pronounced with novel microemulsion vehicles (183.30 ± 156.32 ng/cm2 and 167.39 ± 108.96 ng/cm2 vs. 157.00 ± 114.91 ng/cm2), highlighting the importance of proper selection of experimental conditions when assessing trans(dermal) drug delivery. Consequently, our results suggest that alkyl polyglucoside based microemulsions are promising vehicles worth exploring further for targeted intraderdermal delivery of adapalene in acne treatment.

Keywords:
Adapalene / Alkyl polyglucoside / Decyl glucoside / Differential stripping / Microemulsion
Source:
Journal of Drug Delivery Science and Technology, 2019, 54, 1-12
Funding / projects:
  • Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)

DOI: 10.1016/j.jddst.2019.101245

ISSN: 1773-2247

WoS: 000505159500004

Scopus: 2-s2.0-85071548632
[ Google Scholar ]
9
7
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/3453
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Bubić Pajić, Nataša
AU  - Ilić, Tanja
AU  - Nikolić, Ines
AU  - Dobričić, Vladimir
AU  - Pantelić, Ivana
AU  - Savić, Snežana
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3453
AB  - Aiming to develop biocompatible microemulsions based on natural alkyl polyglucoside surfactant as prospective carriers for improved dermal delivery of adapalene, phase behavior and microstructure of pseudo-ternary oil/decyl glucoside/propylene glycol/water systems were evaluated. The chosen inverted bicontinuous formulations did not change their microstructure upon drug incorporation and remained stable during 1-year period. Preliminary in vivo assessment of skin performances suggested satisfying safety profiles of placebo microemulsions, in spite of considerable changes in skin hydration and barrier function. Interestingly, despite lower in vitro drug release, the amount of adapalene penetrated into porcine skin under infinite dosing regime was higher from microemulsions than from commercial drug product, reaching dermal retention enhancement ratio of 5.9. However, by changing experimental conditions to the more realistic in-use situation, the amount of adapalene extracted from the stratum corneum was comparable for microemulsions and marketed product. Similarly, the drug deposition in hair follicles was slightly pronounced with novel microemulsion vehicles (183.30 ± 156.32 ng/cm2 and 167.39 ± 108.96 ng/cm2 vs. 157.00 ± 114.91 ng/cm2), highlighting the importance of proper selection of experimental conditions when assessing trans(dermal) drug delivery. Consequently, our results suggest that alkyl polyglucoside based microemulsions are promising vehicles worth exploring further for targeted intraderdermal delivery of adapalene in acne treatment.
T2  - Journal of Drug Delivery Science and Technology
T1  - Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form
VL  - 54
SP  - 1
EP  - 12
DO  - 10.1016/j.jddst.2019.101245
ER  - 
@article{
author = "Bubić Pajić, Nataša and Ilić, Tanja and Nikolić, Ines and Dobričić, Vladimir and Pantelić, Ivana and Savić, Snežana",
year = "2019",
abstract = "Aiming to develop biocompatible microemulsions based on natural alkyl polyglucoside surfactant as prospective carriers for improved dermal delivery of adapalene, phase behavior and microstructure of pseudo-ternary oil/decyl glucoside/propylene glycol/water systems were evaluated. The chosen inverted bicontinuous formulations did not change their microstructure upon drug incorporation and remained stable during 1-year period. Preliminary in vivo assessment of skin performances suggested satisfying safety profiles of placebo microemulsions, in spite of considerable changes in skin hydration and barrier function. Interestingly, despite lower in vitro drug release, the amount of adapalene penetrated into porcine skin under infinite dosing regime was higher from microemulsions than from commercial drug product, reaching dermal retention enhancement ratio of 5.9. However, by changing experimental conditions to the more realistic in-use situation, the amount of adapalene extracted from the stratum corneum was comparable for microemulsions and marketed product. Similarly, the drug deposition in hair follicles was slightly pronounced with novel microemulsion vehicles (183.30 ± 156.32 ng/cm2 and 167.39 ± 108.96 ng/cm2 vs. 157.00 ± 114.91 ng/cm2), highlighting the importance of proper selection of experimental conditions when assessing trans(dermal) drug delivery. Consequently, our results suggest that alkyl polyglucoside based microemulsions are promising vehicles worth exploring further for targeted intraderdermal delivery of adapalene in acne treatment.",
journal = "Journal of Drug Delivery Science and Technology",
title = "Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form",
volume = "54",
pages = "1-12",
doi = "10.1016/j.jddst.2019.101245"
}
Bubić Pajić, N., Ilić, T., Nikolić, I., Dobričić, V., Pantelić, I.,& Savić, S.. (2019). Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form. in Journal of Drug Delivery Science and Technology, 54, 1-12.
https://doi.org/10.1016/j.jddst.2019.101245
Bubić Pajić N, Ilić T, Nikolić I, Dobričić V, Pantelić I, Savić S. Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form. in Journal of Drug Delivery Science and Technology. 2019;54:1-12.
doi:10.1016/j.jddst.2019.101245 .
Bubić Pajić, Nataša, Ilić, Tanja, Nikolić, Ines, Dobričić, Vladimir, Pantelić, Ivana, Savić, Snežana, "Alkyl polyglucoside-based adapalene-loaded microemulsions for targeted dermal delivery: Structure, stability and comparative biopharmaceutical characterization with a conventional dosage form" in Journal of Drug Delivery Science and Technology, 54 (2019):1-12,
https://doi.org/10.1016/j.jddst.2019.101245 . .

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