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Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment

Authorized Users Only
2019
Authors
Savić, Vedrana
Ilić, Tanja
Nikolić, Ines
Marković, Bojan
Čalija, Bojan
Cekić, Nebojša
Savić, Snežana
Article (Published version)
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Abstract
Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared ...to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54 ± 92.38 ng/cm2), followed by NE (128.17 ± 48.87 ng/cm2) and Protopic® (77.61 ± 43.25 ng/cm2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.

Keywords:
Capryol™ 90 / Dermal drug delivery / Lecithin-based nanostructured lipid carriers / Nanoemulsion / Precirol® ATO 5 / Tacrolimus
Source:
International Journal of Pharmaceutics, 2019, 569, 1-11
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.ijpharm.2019.118624

ISSN: 0378-5173

WoS: 000488123900053

Scopus: 2-s2.0-85070689387
[ Google Scholar ]
21
11
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/3454
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Savić, Vedrana
AU  - Ilić, Tanja
AU  - Nikolić, Ines
AU  - Marković, Bojan
AU  - Čalija, Bojan
AU  - Cekić, Nebojša
AU  - Savić, Snežana
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3454
AB  - Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54 ± 92.38 ng/cm2), followed by NE (128.17 ± 48.87 ng/cm2) and Protopic® (77.61 ± 43.25 ng/cm2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.
T2  - International Journal of Pharmaceutics
T1  - Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment
VL  - 569
SP  - 1
EP  - 11
DO  - 10.1016/j.ijpharm.2019.118624
ER  - 
@article{
author = "Savić, Vedrana and Ilić, Tanja and Nikolić, Ines and Marković, Bojan and Čalija, Bojan and Cekić, Nebojša and Savić, Snežana",
year = "2019",
abstract = "Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54 ± 92.38 ng/cm2), followed by NE (128.17 ± 48.87 ng/cm2) and Protopic® (77.61 ± 43.25 ng/cm2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.",
journal = "International Journal of Pharmaceutics",
title = "Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment",
volume = "569",
pages = "1-11",
doi = "10.1016/j.ijpharm.2019.118624"
}
Savić, V., Ilić, T., Nikolić, I., Marković, B., Čalija, B., Cekić, N.,& Savić, S.. (2019). Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment. in International Journal of Pharmaceutics, 569, 1-11.
https://doi.org/10.1016/j.ijpharm.2019.118624
Savić V, Ilić T, Nikolić I, Marković B, Čalija B, Cekić N, Savić S. Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment. in International Journal of Pharmaceutics. 2019;569:1-11.
doi:10.1016/j.ijpharm.2019.118624 .
Savić, Vedrana, Ilić, Tanja, Nikolić, Ines, Marković, Bojan, Čalija, Bojan, Cekić, Nebojša, Savić, Snežana, "Tacrolimus-loaded lecithin-based nanostructured lipid carrier and nanoemulsion with propylene glycol monocaprylate as a liquid lipid: Formulation characterization and assessment of dermal delivery compared to referent ointment" in International Journal of Pharmaceutics, 569 (2019):1-11,
https://doi.org/10.1016/j.ijpharm.2019.118624 . .

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