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
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2019
Authors
Savić, VedranaIlić, Tanja

Nikolić, Ines

Marković, Bojan

Čalija, Bojan

Cekić, Nebojša

Savić, Snežana

Article (Published version)

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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 / TacrolimusSource:
International Journal of Pharmaceutics, 2019, 569, 1-11Funding / projects:
DOI: 10.1016/j.ijpharm.2019.118624
ISSN: 0378-5173
WoS: 000488123900053
Scopus: 2-s2.0-85070689387
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PharmacyTY - 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 . .