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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

Само за регистроване кориснике
2015
Аутори
Đekić, Ljiljana
Martinović, Martina
Stepanović-Petrović, Radica
Tomić, Maja
Micov, Ana
Primorac, Marija
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документу
Апстракт
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 (R-0(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 (R-H(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.

Кључне речи:
biocompatibility / controlled release / drug delivery systems / light scattering (dynamic) / microemulsion / nanotechnology / physicochemical properties / polymers / skin
Извор:
Journal of Pharmaceutical Sciences, 2015, 104, 8, 2501-2512
Издавач:
  • Wiley, Hoboken
Финансирање / пројекти:
  • Развој производа и технологија које обезбеђују жељено ослобађање лековитих супстанци из чврстих фармацеутских облика (RS-34007)

DOI: 10.1002/jps.24494

ISSN: 0022-3549

PubMed: 26045240

WoS: 000358009700012

Scopus: 2-s2.0-84947047528
[ Google Scholar ]
19
18
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2426
Колекције
  • Radovi istraživača / Researchers’ publications
Институција/група
Pharmacy
TY  - JOUR
AU  - Đekić, Ljiljana
AU  - Martinović, Martina
AU  - Stepanović-Petrović, Radica
AU  - Tomić, Maja
AU  - Micov, Ana
AU  - Primorac, Marija
PY  - 2015
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2426
AB  - 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 (R-0(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 (R-H(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.
PB  - Wiley, Hoboken
T2  - Journal of Pharmaceutical Sciences
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
VL  - 104
IS  - 8
SP  - 2501
EP  - 2512
DO  - 10.1002/jps.24494
ER  - 
@article{
author = "Đekić, Ljiljana and Martinović, Martina and Stepanović-Petrović, Radica and Tomić, Maja and Micov, Ana and Primorac, Marija",
year = "2015",
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 (R-0(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 (R-H(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.",
publisher = "Wiley, Hoboken",
journal = "Journal of Pharmaceutical Sciences",
title = "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",
volume = "104",
number = "8",
pages = "2501-2512",
doi = "10.1002/jps.24494"
}
Đekić, L., Martinović, 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. in Journal of Pharmaceutical Sciences
Wiley, Hoboken., 104(8), 2501-2512.
https://doi.org/10.1002/jps.24494
Đekić L, Martinović M, Stepanović-Petrović R, Tomić M, Micov A, Primorac M. 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. in Journal of Pharmaceutical Sciences. 2015;104(8):2501-2512.
doi:10.1002/jps.24494 .
Đekić, Ljiljana, Martinović, Martina, Stepanović-Petrović, Radica, Tomić, Maja, Micov, Ana, Primorac, Marija, "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" in Journal of Pharmaceutical Sciences, 104, no. 8 (2015):2501-2512,
https://doi.org/10.1002/jps.24494 . .

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