Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-β-cyclodextrin

Medarević, Djordje; Kachrimanis, Kyriakos; Djurić, Z.; Ibrić, Svetlana

doi:10.1016/j.ejps.2015.08.001

Cited by 51 publications

(32 citation statements)

References 36 publications

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“…The solubilizing effect of BCD was increased in the presence of CMC; consequently, a synergistic effect in SLM solubility was observed in the presence of BCD and CMC. In the present work addition of small amount of hydrophilic polymer such as CMC to cyclodextrin solution resulted in significant improvement in the complexation efficiency between SLM-BCD thereby markedly enhancing the solubilizing efficiency of BCD and this is in agreement with previous reports [19][20][21][22][23][24][25][26][27] . In vitro studies in distilled water for inclusion complexes of BCD with CMC showed higher rate of dissolution than those of SLM alone and its binary complexes with BCD.…”

Section: Discussionsupporting

confidence: 81%

“…Addition of small amounts of water soluble polymers to the drug cyclodextrin binary systems are known to improve both the complexing and solubilizing efficiencies of cyclodextrins [19][20][21][22] . Ternary inclusion complexes of beta-cyclodextrin derivatives with sodium carboxymethyl cellulose (CMC) with have been reported for Rofecoxib 23 , Nimuselide 24 , cefpodoxime 25 , Budesonide 26 and Tropicamide 27 in order to improve their solubility or therapeutic responses.…”

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confidence: 99%

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2016

IJPSR

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ABSTRACT:The objective of the present investigation was to study the complexation of silymarin, a poorly water soluble herbal drug, with β-cyclodextrin alone and in the presence of sodium carboxymethyl cellulose to evaluate the feasibility of enhancing the solubility and dissolution rate of silymarine. Phase solubility study and kneading method was employed to develop and formulate solid inclusion complexes. Solid inclusion complexes of silymarin -β-cyclodextrin in 1:1 molar ratio were prepared with and without carboxymethyl cellulose by kneading method. Obtained binary and ternary complexes were evaluated for solubility dissolution and physical nature by FTIR, XRD and NMR. The aqueous solubility of silymarin was linearly increased as a function of the concentration of β-cyclodextrin alone and in the presence of sodium carboxymethyl cellulose. Beta cyclodextrin formed binary molecular inclusion complexes with silymarin in1:1 molar ratio as revealed by phase solubility diagram. Sodium carboxymethyl cellulose in ternary complexes has resulted in 2.37 and 1.66 fold enhancements in complexation and solubilizing efficiencies of β-cyclodextrin respectively. Dissolution rate of silymarin in binary and ternary complexes was enhanced up to 1.3 and 1.6 folds respectively when compared with pure silymarin. It is evident that addition of sodium carboxymethyl cellulose affects the complexation and solubilizing efficiencies of β-cyclodextrin hence it may be used in solid dispersions to minimize the overall formulation bulk.

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Section: Discussionsupporting

confidence: 81%

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confidence: 99%

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2016

IJPSR

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“…The smallest cavity of the a-CD (0.5-0.6 nm) compared to the one of the b-CD (0.6-0.8 nm) facilitates the closeness of atoms, and consequently, the formation of steric, mainly, but also hydrogen bonds that corroborates with the DH value. Negative values of DH indicated hydrophobic non-covalent interactions, which may be stabilized by hydrogen bonding, as it was confirmed by the molecular docking [53,54]. The Fig.…”

Section: Molecular Docking Between A- B-cd and Isopsupporting

confidence: 55%

Docking and physico-chemical properties of α- and β-cyclodextrin complex containing isopulegol: a comparative study

Menezes

Dória

Araújo

et al. 2016

J Incl Phenom Macrocycl Chem

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Isopulegol (ISOP) is a monoterpenoid alcohol presented in the essential oils of several plants that possesses therapeutic properties The aim of this work was prepare samples with ISOP and a-and b-cyclodextrins (aand b-CD) through three different methods: physical mixture, paste method (PC) and slurry complexation (SC). In order to evaluate the formation of inclusion complexes, the techniques of differential scanning calorimetry, thermogravimetry/derivative thermogravimetry, fourier transform infrared spectroscopy, X-ray diffractometry (XRD), gas chromatography-mass spectrometry analyses (GC/ MS), docking, nuclear magnetic resonance and scanning electron microscopy were considered. The analyses of the a-CD or b-CD/ISOP revealed the formation of a complex mainly through the PC and SC methods for a-CD and b-CD, respectively. XRD diffraction characteristics presented formation of a trend to new solid phase, which suggested the formation of inclusion complexes. The GC/MS demonstrated that the PC method was the best one to form complexation with a-CD (48.8 %). Concerning b-CD, the SC method exhibited the strongest complexation (68.3 %). Furthermore, the molecular theoretical docking study demonstrated that a-CD/ISOP inclusion complex formed a more stable complex than did the b-CD/ISOP inclusion complex.

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“…The fast dissolution of ITZ in vitro was attributed to the high hydrophilicity of CD and to the stabilization of the complex due to the presence of the polymer. Indeed, Medarevic et al pointed out that adding a hydrophilic polymer, such as SOL, increases the stability of the inclusion complex in vitro (Medarevic et al, 2015). However, the gastro-intestinal fluids are much more complex than a simple aqueous medium.…”

Section: In Vivo Assessment Of Bioavailability Enhancementmentioning

confidence: 99%