Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen
Abstract
Suitability of liquid lecithin (i.e., solution of lecithin in soy bean oil with similar to 60% w/w of phospholipids) for formation of gels, upon addition of water solution of poloxamer 407, was investigated, and formulated systems were evaluated as carriers for percutaneous delivery of ibuprofen. Formulation study of pseudoternary system liquid lecithin/poloxamer 407/water at constant liquid lecithin/poloxamer 407 mass ratio (2.0) revealed that minimum concentrations of liquid lecithin and poloxamer 407 required for formation of gel like systems were 15.75% w/w and 13.13% w/w, respectively, while the maximum content of water was 60.62% w/w. The systems comprising water concentrations in a range from 55 to 60.62% w/w were soft semisolids suitable for topical application, and they were selected for physicochemical and biopharmaceutical evaluation. Analysis of conductivity results and light microscopy examination revealed that investigated systems were water dilutable dispersions of spher...ical oligolamellar associates of phospholipids and triglyceride molecules in the copolymer water solution. Rheological behavior evaluation results indicated that the investigated gels were thermosensitive shear thinning systems. Ibuprofen (5% w/w) was incorporated by dispersing into the previously prepared carriers. Drug-loaded systems were physically stable at storage temperature from 5 +/- 3 degrees C to 40 +/- 2 degrees C, for 30 days. In vitro ibuprofen release was in accordance with the Higuchi model (r(H) > 0.95) and sustained for 12 h. The obtained results implicated that formulated LLPBGs, optimized regarding drug release and organoleptic properties, represent promising carriers for sustained percutaneous drug delivery of poorly soluble drugs.
Keywords:
Liquid lecithin / Poloxamer 407 / Thermosensitive gels / Gelation process / Sustained drug release / IbuprofenSource:
International Journal of Pharmaceutics, 2015, 490, 1-2, 180-189Publisher:
- Elsevier Science BV, Amsterdam
Funding / projects:
DOI: 10.1016/j.ijpharm.2015.05.040
ISSN: 0378-5173
PubMed: 26002567
WoS: 000356836700021
Scopus: 2-s2.0-84931275476
Collections
Institution/Community
PharmacyTY - JOUR AU - Đekić, Ljiljana AU - Krajišnik, Danina AU - Martinović, Martina AU - Đorđević, Dragana AU - Primorac, Marija PY - 2015 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2468 AB - Suitability of liquid lecithin (i.e., solution of lecithin in soy bean oil with similar to 60% w/w of phospholipids) for formation of gels, upon addition of water solution of poloxamer 407, was investigated, and formulated systems were evaluated as carriers for percutaneous delivery of ibuprofen. Formulation study of pseudoternary system liquid lecithin/poloxamer 407/water at constant liquid lecithin/poloxamer 407 mass ratio (2.0) revealed that minimum concentrations of liquid lecithin and poloxamer 407 required for formation of gel like systems were 15.75% w/w and 13.13% w/w, respectively, while the maximum content of water was 60.62% w/w. The systems comprising water concentrations in a range from 55 to 60.62% w/w were soft semisolids suitable for topical application, and they were selected for physicochemical and biopharmaceutical evaluation. Analysis of conductivity results and light microscopy examination revealed that investigated systems were water dilutable dispersions of spherical oligolamellar associates of phospholipids and triglyceride molecules in the copolymer water solution. Rheological behavior evaluation results indicated that the investigated gels were thermosensitive shear thinning systems. Ibuprofen (5% w/w) was incorporated by dispersing into the previously prepared carriers. Drug-loaded systems were physically stable at storage temperature from 5 +/- 3 degrees C to 40 +/- 2 degrees C, for 30 days. In vitro ibuprofen release was in accordance with the Higuchi model (r(H) > 0.95) and sustained for 12 h. The obtained results implicated that formulated LLPBGs, optimized regarding drug release and organoleptic properties, represent promising carriers for sustained percutaneous drug delivery of poorly soluble drugs. PB - Elsevier Science BV, Amsterdam T2 - International Journal of Pharmaceutics T1 - Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen VL - 490 IS - 1-2 SP - 180 EP - 189 DO - 10.1016/j.ijpharm.2015.05.040 ER -
@article{ author = "Đekić, Ljiljana and Krajišnik, Danina and Martinović, Martina and Đorđević, Dragana and Primorac, Marija", year = "2015", abstract = "Suitability of liquid lecithin (i.e., solution of lecithin in soy bean oil with similar to 60% w/w of phospholipids) for formation of gels, upon addition of water solution of poloxamer 407, was investigated, and formulated systems were evaluated as carriers for percutaneous delivery of ibuprofen. Formulation study of pseudoternary system liquid lecithin/poloxamer 407/water at constant liquid lecithin/poloxamer 407 mass ratio (2.0) revealed that minimum concentrations of liquid lecithin and poloxamer 407 required for formation of gel like systems were 15.75% w/w and 13.13% w/w, respectively, while the maximum content of water was 60.62% w/w. The systems comprising water concentrations in a range from 55 to 60.62% w/w were soft semisolids suitable for topical application, and they were selected for physicochemical and biopharmaceutical evaluation. Analysis of conductivity results and light microscopy examination revealed that investigated systems were water dilutable dispersions of spherical oligolamellar associates of phospholipids and triglyceride molecules in the copolymer water solution. Rheological behavior evaluation results indicated that the investigated gels were thermosensitive shear thinning systems. Ibuprofen (5% w/w) was incorporated by dispersing into the previously prepared carriers. Drug-loaded systems were physically stable at storage temperature from 5 +/- 3 degrees C to 40 +/- 2 degrees C, for 30 days. In vitro ibuprofen release was in accordance with the Higuchi model (r(H) > 0.95) and sustained for 12 h. The obtained results implicated that formulated LLPBGs, optimized regarding drug release and organoleptic properties, represent promising carriers for sustained percutaneous drug delivery of poorly soluble drugs.", publisher = "Elsevier Science BV, Amsterdam", journal = "International Journal of Pharmaceutics", title = "Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen", volume = "490", number = "1-2", pages = "180-189", doi = "10.1016/j.ijpharm.2015.05.040" }
Đekić, L., Krajišnik, D., Martinović, M., Đorđević, D.,& Primorac, M.. (2015). Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen. in International Journal of Pharmaceutics Elsevier Science BV, Amsterdam., 490(1-2), 180-189. https://doi.org/10.1016/j.ijpharm.2015.05.040
Đekić L, Krajišnik D, Martinović M, Đorđević D, Primorac M. Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen. in International Journal of Pharmaceutics. 2015;490(1-2):180-189. doi:10.1016/j.ijpharm.2015.05.040 .
Đekić, Ljiljana, Krajišnik, Danina, Martinović, Martina, Đorđević, Dragana, Primorac, Marija, "Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen" in International Journal of Pharmaceutics, 490, no. 1-2 (2015):180-189, https://doi.org/10.1016/j.ijpharm.2015.05.040 . .