Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design
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2016
Authors
Isailović, TanjaĐorđević, Sanela
Marković, Bojan
Randelović, Danijela
Cekić, Nebojša
Lukić, Milica
Pantelić, Ivana
Daniels, Rolf
Savić, Snežana
Article (Published version)
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We aimed to develop lecithin-based nanoemulsions intended for effective aceclofenac (ACF) skin delivery utilizing sucrose esters [sucrose palmitate (SP) and sucrose stearate (SS)] as additional stabilizers and penetration enhancers. To find the suitable surfactant mixtures and levels of process variables (homogenization pressure and number of cycles-high pressure homogenization manufacturing method) that result in drug-loaded nanoemulsions with minimal droplet size and narrow size distribution, a combined mixture-process experimental design was employed. Based on optimization data, selected nanoemulsions were evaluated regarding morphology, surface charge, drug-excipient interactions, physical stability, and in vivo skin performances (skin penetration and irritation potential). The predicted physicochemical properties and storage stability were proved satisfying for ACF-loaded nanoemulsions containing 2% of SP in the blend with 0%-1% of SS and 1%-2% of egg lecithin (produced at 50 degr...ees C/20 cycles/800 bar). Additionally, the in vivo tape stripping demonstrated superior ACF skin absorption from these nanoemulsions, particularly from those containing 2% of SP, 0.5% of SS, and 1.5% of egg lecithin, when comparing with the sample costabilized by conventional surfactant-polysorbate 80. In summary, the combined mixture-process experimental design was shown as a feasible tool for formulation development of multisurfactant-based nanosized delivery systems with potentially improved overall product performances.
Source:
Journal of Pharmaceutical Sciences, 2016, 105, 1, 308-323Publisher:
- Elsevier Science Inc, New York
Funding / projects:
- Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-MESTD-Technological Development (TD or TR)-34031)
DOI: 10.1002/jps.24706
ISSN: 0022-3549
PubMed: 26539935
WoS: 000381768000038
Scopus: 2-s2.0-84964478863
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Institution/Community
PharmacyTY - JOUR AU - Isailović, Tanja AU - Đorđević, Sanela AU - Marković, Bojan AU - Randelović, Danijela AU - Cekić, Nebojša AU - Lukić, Milica AU - Pantelić, Ivana AU - Daniels, Rolf AU - Savić, Snežana PY - 2016 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2716 AB - We aimed to develop lecithin-based nanoemulsions intended for effective aceclofenac (ACF) skin delivery utilizing sucrose esters [sucrose palmitate (SP) and sucrose stearate (SS)] as additional stabilizers and penetration enhancers. To find the suitable surfactant mixtures and levels of process variables (homogenization pressure and number of cycles-high pressure homogenization manufacturing method) that result in drug-loaded nanoemulsions with minimal droplet size and narrow size distribution, a combined mixture-process experimental design was employed. Based on optimization data, selected nanoemulsions were evaluated regarding morphology, surface charge, drug-excipient interactions, physical stability, and in vivo skin performances (skin penetration and irritation potential). The predicted physicochemical properties and storage stability were proved satisfying for ACF-loaded nanoemulsions containing 2% of SP in the blend with 0%-1% of SS and 1%-2% of egg lecithin (produced at 50 degrees C/20 cycles/800 bar). Additionally, the in vivo tape stripping demonstrated superior ACF skin absorption from these nanoemulsions, particularly from those containing 2% of SP, 0.5% of SS, and 1.5% of egg lecithin, when comparing with the sample costabilized by conventional surfactant-polysorbate 80. In summary, the combined mixture-process experimental design was shown as a feasible tool for formulation development of multisurfactant-based nanosized delivery systems with potentially improved overall product performances. PB - Elsevier Science Inc, New York T2 - Journal of Pharmaceutical Sciences T1 - Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design VL - 105 IS - 1 SP - 308 EP - 323 DO - 10.1002/jps.24706 ER -
@article{ author = "Isailović, Tanja and Đorđević, Sanela and Marković, Bojan and Randelović, Danijela and Cekić, Nebojša and Lukić, Milica and Pantelić, Ivana and Daniels, Rolf and Savić, Snežana", year = "2016", abstract = "We aimed to develop lecithin-based nanoemulsions intended for effective aceclofenac (ACF) skin delivery utilizing sucrose esters [sucrose palmitate (SP) and sucrose stearate (SS)] as additional stabilizers and penetration enhancers. To find the suitable surfactant mixtures and levels of process variables (homogenization pressure and number of cycles-high pressure homogenization manufacturing method) that result in drug-loaded nanoemulsions with minimal droplet size and narrow size distribution, a combined mixture-process experimental design was employed. Based on optimization data, selected nanoemulsions were evaluated regarding morphology, surface charge, drug-excipient interactions, physical stability, and in vivo skin performances (skin penetration and irritation potential). The predicted physicochemical properties and storage stability were proved satisfying for ACF-loaded nanoemulsions containing 2% of SP in the blend with 0%-1% of SS and 1%-2% of egg lecithin (produced at 50 degrees C/20 cycles/800 bar). Additionally, the in vivo tape stripping demonstrated superior ACF skin absorption from these nanoemulsions, particularly from those containing 2% of SP, 0.5% of SS, and 1.5% of egg lecithin, when comparing with the sample costabilized by conventional surfactant-polysorbate 80. In summary, the combined mixture-process experimental design was shown as a feasible tool for formulation development of multisurfactant-based nanosized delivery systems with potentially improved overall product performances.", publisher = "Elsevier Science Inc, New York", journal = "Journal of Pharmaceutical Sciences", title = "Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design", volume = "105", number = "1", pages = "308-323", doi = "10.1002/jps.24706" }
Isailović, T., Đorđević, S., Marković, B., Randelović, D., Cekić, N., Lukić, M., Pantelić, I., Daniels, R.,& Savić, S.. (2016). Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design. in Journal of Pharmaceutical Sciences Elsevier Science Inc, New York., 105(1), 308-323. https://doi.org/10.1002/jps.24706
Isailović T, Đorđević S, Marković B, Randelović D, Cekić N, Lukić M, Pantelić I, Daniels R, Savić S. Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design. in Journal of Pharmaceutical Sciences. 2016;105(1):308-323. doi:10.1002/jps.24706 .
Isailović, Tanja, Đorđević, Sanela, Marković, Bojan, Randelović, Danijela, Cekić, Nebojša, Lukić, Milica, Pantelić, Ivana, Daniels, Rolf, Savić, Snežana, "Biocompatible Nanoemulsions for Improved Aceclofenac Skin Delivery: Formulation Approach Using Combined Mixture-Process Experimental Design" in Journal of Pharmaceutical Sciences, 105, no. 1 (2016):308-323, https://doi.org/10.1002/jps.24706 . .