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Dissolution rate enhancement and physicochemical characterization of carbamazepine-poloxamer solid dispersions.
Pharm Dev Technol. 2016; 21(3):268-76.PD

Abstract

This study investigates the potential of poloxamers as solid dispersions (SDs) carriers in improving the dissolution rate of a poorly soluble drug, carbamazepine (CBZ). Solid dispersions were prepared with poloxamer 188 (P188) and poloxamer 407 (P407) by melting method in different drug:carrier ratios (1:1, 1:2 and 1:3). Prepared samples were characterized using differential scanning calorimetry (DSC), hot-stage polarized light microscopy (HSM), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FT-IR) to investigate drug physical state within the SDs matrix, possible polymorphic transitions and drug-polymer interactions. The interactions between CBZ molecules and polymeric chains were also evaluated using molecular dynamics simulation (MDS) technique. The most thermodynamically stable polymorphic form III of CBZ was present in all SDs, regardless of the type of poloxamer and drug-to-carrier ratio. The absence of drug-polymer interactions was observed by FT-IR analysis and additionally confirmed by MDS. Formation of persistent hydrogen bond between two CBZ molecules, observed by MDS indicate high tendency of CBZ molecules to aggregate and form crystalline phase within dispersion. P188 exhibit higher efficiency in increasing CBZ dissolution rate due to its more pronounced hydrophilic properties, while increasing poloxamers concentration resulted in decreasing drug release rate, as a consequence of their thermoreversible gelation.

Authors+Show Affiliations

a Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy , University of Belgrade , Belgrade , Serbia .b Department of Pharmaceutical Technology, Faculty of Pharmacy , Aristotle University of Thessaloniki , Thessaloniki , Greece , and.c Vinča Institute of Nuclear Sciences, University of Belgrade , Belgrade , Serbia.a Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy , University of Belgrade , Belgrade , Serbia .a Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy , University of Belgrade , Belgrade , Serbia .a Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy , University of Belgrade , Belgrade , Serbia .

Pub Type(s)

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

Language

eng

PubMed ID

25582577

Citation

Medarević, Djordje P., et al. "Dissolution Rate Enhancement and Physicochemical Characterization of Carbamazepine-poloxamer Solid Dispersions." Pharmaceutical Development and Technology, vol. 21, no. 3, 2016, pp. 268-76.
Medarević DP, Kachrimanis K, Mitrić M, et al. Dissolution rate enhancement and physicochemical characterization of carbamazepine-poloxamer solid dispersions. Pharm Dev Technol. 2016;21(3):268-76.
Medarević, D. P., Kachrimanis, K., Mitrić, M., Djuriš, J., Djurić, Z., & Ibrić, S. (2016). Dissolution rate enhancement and physicochemical characterization of carbamazepine-poloxamer solid dispersions. Pharmaceutical Development and Technology, 21(3), 268-76. https://doi.org/10.3109/10837450.2014.996899
Medarević DP, et al. Dissolution Rate Enhancement and Physicochemical Characterization of Carbamazepine-poloxamer Solid Dispersions. Pharm Dev Technol. 2016;21(3):268-76. PubMed PMID: 25582577.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Dissolution rate enhancement and physicochemical characterization of carbamazepine-poloxamer solid dispersions. AU - Medarević,Djordje P, AU - Kachrimanis,Kyriakos, AU - Mitrić,Miodrag, AU - Djuriš,Jelena, AU - Djurić,Zorica, AU - Ibrić,Svetlana, Y1 - 2015/01/13/ PY - 2015/1/14/entrez PY - 2015/1/15/pubmed PY - 2016/11/12/medline KW - Carbamazepine KW - dissolution rate KW - molecular dynamics KW - physicochemical characterization KW - poloxamers KW - solid dispersions SP - 268 EP - 76 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 21 IS - 3 N2 - This study investigates the potential of poloxamers as solid dispersions (SDs) carriers in improving the dissolution rate of a poorly soluble drug, carbamazepine (CBZ). Solid dispersions were prepared with poloxamer 188 (P188) and poloxamer 407 (P407) by melting method in different drug:carrier ratios (1:1, 1:2 and 1:3). Prepared samples were characterized using differential scanning calorimetry (DSC), hot-stage polarized light microscopy (HSM), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FT-IR) to investigate drug physical state within the SDs matrix, possible polymorphic transitions and drug-polymer interactions. The interactions between CBZ molecules and polymeric chains were also evaluated using molecular dynamics simulation (MDS) technique. The most thermodynamically stable polymorphic form III of CBZ was present in all SDs, regardless of the type of poloxamer and drug-to-carrier ratio. The absence of drug-polymer interactions was observed by FT-IR analysis and additionally confirmed by MDS. Formation of persistent hydrogen bond between two CBZ molecules, observed by MDS indicate high tendency of CBZ molecules to aggregate and form crystalline phase within dispersion. P188 exhibit higher efficiency in increasing CBZ dissolution rate due to its more pronounced hydrophilic properties, while increasing poloxamers concentration resulted in decreasing drug release rate, as a consequence of their thermoreversible gelation. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/25582577/Dissolution_rate_enhancement_and_physicochemical_characterization_of_carbamazepine_poloxamer_solid_dispersions_ L2 - http://www.tandfonline.com/doi/full/10.3109/10837450.2014.996899 DB - PRIME DP - Unbound Medicine ER -