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Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions
dc.creator | Đekić, Ljiljana | |
dc.creator | Primorac, Marija | |
dc.creator | Filipić, Slavica | |
dc.creator | Agbaba, Danica | |
dc.date.accessioned | 2019-09-02T11:29:47Z | |
dc.date.available | 2019-09-02T11:29:47Z | |
dc.date.issued | 2012 | |
dc.identifier.issn | 0378-5173 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/1736 | |
dc.description.abstract | The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol (R)). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma (R) 2421 and Solubilisant gamma (R) 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol (R)/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (K-m) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1-M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief (R), Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70-6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and K-m value. Solubilisant gamma (R) 2429 as well as higher K-m (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly solubilized within the interface film. The amount of drug released from the formulations M3 (10.75%, w/w) and M6 (13.45%, w/w) (K-m 60: 40) was limited in comparison with the reference (22.22%, w/w) and follows the Higuchi model. Microemulsions M2 and M5 (K-m 50: 50) gave zero order drug release pattern and similar to 15% (w/w) ibuprofen released. The release profiles from microemulsions M1 and M4 (K-m 40: 60) did not fit well with the models used for analysis, although the amounts of ibuprofen released (24.47%, w/w) and 17.99% (w/w), respectively) were comparable to that of the reference hydrogel. The drug release mechanism was related with the surfactant/cosurfactant synergism, thus the lower efficiency of the tensides corresponded to the faster drug release. | en |
dc.publisher | Elsevier Science BV, Amsterdam | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/46010/RS// | |
dc.rights | restrictedAccess | |
dc.source | International Journal of Pharmaceutics | |
dc.subject | Microemulsions | en |
dc.subject | Surfactant/cosurfactant synergism | en |
dc.subject | Drug solubilization capacity | en |
dc.subject | In vitro release testing (IVRT) | en |
dc.subject | Ibuprofen | en |
dc.title | Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Филипић, Славица; Aгбаба, Даница; Ђекић, Љиљана; Приморац, Марија; | |
dc.citation.volume | 433 | |
dc.citation.issue | 1-2 | |
dc.citation.spage | 25 | |
dc.citation.epage | 33 | |
dc.citation.other | 433(1-2): 25-33 | |
dc.citation.rank | M21 | |
dc.identifier.wos | 000305420100004 | |
dc.identifier.doi | 10.1016/j.ijpharm.2012.04.070 | |
dc.identifier.pmid | 22579578 | |
dc.identifier.scopus | 2-s2.0-84862848717 | |
dc.type.version | publishedVersion |