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Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration.
J Pharm Sci. 2015 Aug; 104(8):2501-12.JP

Abstract

Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-in-water microemulsions with Newtonian flow behavior, low viscosity (from 368 ± 38 to 916 ± 46 mPa s), and average droplet size from 14.79 ± 0.31 to 16.54 ± 0.75 nm. Ibuprofen in vitro release from the microemulsions was in accordance with zero-order kinetics (R0(2) > 0.99) for at least 12 h. The maximum drug release rate (3.55%h(-1)) was from the microemulsion M3 comprising 16%, w/w of poloxamer 407. The release rate of ibuprofen from the reference hydrogel followed Higuchi kinetics (RH(2) > 0.99), and drug amount released after the 6th hour was negligible. In a rat model of inflammation, the microemulsion M3 was significantly more efficacious than the reference hydrogel in exerting antihyperalgesic effects in prophylactic topical treatment, whereas they were comparable in therapeutic treatment as well as in producing antiedematous effect in both protocols. No obvious skin irritation was observed in in vivo studies. The developed nonionic surfactants-based microemulsions containing the optimal concentration of poloxamer 407 could be promising carriers for sustained regional delivery of ibuprofen via topical administration.

Authors+Show Affiliations

Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.Department of Pharmacology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.Department of Pharmacology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.Department of Pharmacology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, 11221, Serbia.

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26045240

Citation

Djekic, Ljiljana, et al. "Design of Block Copolymer Costabilized Nonionic Microemulsions and Their in Vitro and in Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen Via Topical Administration." Journal of Pharmaceutical Sciences, vol. 104, no. 8, 2015, pp. 2501-12.
Djekic L, Martinovic M, Stepanović-Petrović R, et al. Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration. J Pharm Sci. 2015;104(8):2501-12.
Djekic, L., Martinovic, M., Stepanović-Petrović, R., Tomić, M., Micov, A., & Primorac, M. (2015). Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration. Journal of Pharmaceutical Sciences, 104(8), 2501-12. https://doi.org/10.1002/jps.24494
Djekic L, et al. Design of Block Copolymer Costabilized Nonionic Microemulsions and Their in Vitro and in Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen Via Topical Administration. J Pharm Sci. 2015;104(8):2501-12. PubMed PMID: 26045240.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration. AU - Djekic,Ljiljana, AU - Martinovic,Martina, AU - Stepanović-Petrović,Radica, AU - Tomić,Maja, AU - Micov,Ana, AU - Primorac,Marija, Y1 - 2015/06/04/ PY - 2015/02/14/received PY - 2015/04/22/revised PY - 2015/04/22/accepted PY - 2015/6/6/entrez PY - 2015/6/6/pubmed PY - 2016/6/3/medline KW - biocompatibility KW - controlled release KW - drug delivery systems KW - light scattering (dynamic) KW - microemulsion KW - nanotechnology KW - physicochemical properties KW - polymers KW - skin SP - 2501 EP - 12 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 104 IS - 8 N2 - Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-in-water microemulsions with Newtonian flow behavior, low viscosity (from 368 ± 38 to 916 ± 46 mPa s), and average droplet size from 14.79 ± 0.31 to 16.54 ± 0.75 nm. Ibuprofen in vitro release from the microemulsions was in accordance with zero-order kinetics (R0(2) > 0.99) for at least 12 h. The maximum drug release rate (3.55%h(-1)) was from the microemulsion M3 comprising 16%, w/w of poloxamer 407. The release rate of ibuprofen from the reference hydrogel followed Higuchi kinetics (RH(2) > 0.99), and drug amount released after the 6th hour was negligible. In a rat model of inflammation, the microemulsion M3 was significantly more efficacious than the reference hydrogel in exerting antihyperalgesic effects in prophylactic topical treatment, whereas they were comparable in therapeutic treatment as well as in producing antiedematous effect in both protocols. No obvious skin irritation was observed in in vivo studies. The developed nonionic surfactants-based microemulsions containing the optimal concentration of poloxamer 407 could be promising carriers for sustained regional delivery of ibuprofen via topical administration. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/26045240/Design_of_Block_Copolymer_Costabilized_Nonionic_Microemulsions_and_Their_In_Vitro_and_In_Vivo_Assessment_as_Carriers_for_Sustained_Regional_Delivery_of_Ibuprofen_via_Topical_Administration_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)30005-8 DB - PRIME DP - Unbound Medicine ER -