Cyclodextrin/imatinib complexation: Binding mode and charge dependent stabilities

Béni, Szabolcs; Szakács, Zoltán; Csernák, Orsolya; Barcza, Lajos; Noszál, Béla

doi:10.1016/j.ejps.2006.10.008

Cited by 59 publications

(29 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…So the rank order in term of solubility enhancement of prednisolone is HP β-CD followed by HPMC and PVP independent of method used for preparing such complexes. Similar observation was also reported in literature where inclusion of poorly soluble drug with cyclodextrin has increased solubility by 10 fold in case of imatinib, [21] 11 fold in case of furosemide [22] while just 4.5 fold increase in solubility was observed for bupivacaine, [23] so it seems to be dependent on the molecular interaction of cyclodextrin and drug.…”

Section: Resultssupporting

confidence: 90%

Delivering drug-polymer complex via quick dissolving film: A step towards the development of an appropriate pediatric formulation

Patel¹,

Patel²

2013

Asian J Pharm

View full text Add to dashboard Cite

L ack of suitable prednisolone formulations for treatment of asthma could limit treatment compliance in pediatric population and hence the aim of this study was to develop prednisolone-polymer complexes with enhanced solubility and to incorporate this complex into orally disintegrating films to enable rapid drug delivery. The prednisolone-polymeric complexes were prepared using solvent evaporation and freeze drying techniques with a drug-polymer ratio of 1:1 using hydroxypropyl β-cyclodextrin (HP β-CD), hydroxypropyl methylcellulose 4 cps, and polyvinylpyrrolidone K-30 as polymeric carriers and the parameters such as an aqueous solubility, dissolution profile, and solid-state characterization using differential scanning calorimetry (DSC) of the complexes determined. The optimized complex was then incorporated into films prepared using solvent casting technique and the weight variation, thickness, solid-state characterization, in vitro disintegration and dissolution profiles of the films were then determined. The highest prednisolone solubility was seen with the prednisolone-HP β-CD complex prepared by freeze drying (1.82 mg/mL) followed by the same complex prepared by solvent evaporation (1.70 mg/mL). The solubility's were significantly higher compared to prednisolone powder (0.2 mg/mL) (P < 0.05). DSC analysis of complexes revealed a reduction in area of the endothermic peak indicating the presence of amorphous drug while in comparison, the DSC analysis of films did not show endothermic peak showing complete absence of crystalline drug. The film was thin, uniform in weight and thickness, showing rapid disintegration of 55 s with almost complete drug release within 3 min. The study revealed the incorporated drug-polymer complex have maintained the amorphous state and enabled rapid drug release.

show abstract

Section: Resultssupporting

confidence: 90%

Delivering drug-polymer complex via quick dissolving film: A step towards the development of an appropriate pediatric formulation

Patel¹,

Patel²

2013

Asian J Pharm

View full text Add to dashboard Cite

show abstract

“…From the viewpoint of encapsulation, intermolecular cross-peaks of the 4-hydroxyphenyl dublets with the inner CD protons H-5 (at 3.88 ppm) and H-3 (at 3.97 ppm) are important. The relative cross-peak intensities revealed that the whole aromatic ring is in the ␤-CD cavity and the mode of penetration occurred from the wider rim side, similar to our previous findings in case of imatinib [24]. A further evidence for this type of orientation of genistein is a weak cross-peak between the ring B singulet (7.96 ppm) and the H-5 proton of ␤-CD (3.88 ppm).…”

Section: Structural Considerations Of the Molecular Encapsulation Ofsupporting

confidence: 86%

Utility of cyclodextrins in the formulation of genistein

Daruházi

Szente

Balogh

et al. 2008

Journal of Pharmaceutical and Biomedical Analysis

Self Cite

View full text Add to dashboard Cite

“…Their cavities with appropriate sizes enable them to form inclusion complex supermolecules with various kinds of hydrophobic drugs, and result in an improvement of the properties of drugs such as solubility, chemical stability, bioavailability, drug-controlled release, or even elimination of drug's abnormal flavour. Therefore the CDs possess good application prospects in oral administration preparation [2,[36][37][38] , and they have also become the important useful functional excipients in modern pharmaceuticals due to the features of CD with easiness to obtain, better biocompatibility, nearly no adverse effects and stable chemical properties as well as clathration simplicity with guest drugs.…”

Section: Cyclodextrin-based Supermolecules As Antitumor Agentsmentioning

confidence: 99%

Review on supermolecules as chemical drugs

Zhou

Gan

Zhang

et al. 2009

Sci. China Ser. B-Chem.

View full text Add to dashboard Cite

Supramolecular medicinal chemistry field has been a quite rapidly developing, increasingly active and newly rising interdiscipline which is the new expansion of supramolecular chemistry in pharmaceutical sciences, and is gradually becoming a relatively independent scientific area. Supramolecular drugs could be defined as medicinal supermolecules formed by two or more molecules through noncovalent bonds. So far a lot of supermolecules as chemical drugs have been widely used in clinics. Supermolecules as chemical drugs, i.e. supramolecular chemical drugs or supramolecular drugs, which might have the excellences of lower cost, shorter period, higher potential as clinical drugs for their successful research and development, may possess higher bioavailability, better biocompatibility and drug-targeting, fewer multidrug-resistances, lower toxicity, less adverse effect, and better curative effects as well as safety, and therefore exhibit wide potential application. These overwhelming advantages have drawn enormous special attention. This paper gives the definition of supramolecular drugs, proposes the concept of supramolecular chemical drugs, and systematically reviews the recent advances in the research and development of supermolecules, including organic and inorganic complex ones as chemical drugs in the area of antitumor, anti-inflammatory, analgesic, antimalarial, antibacterial, antifungal, antivirus, anti-epileptic, cardiovascular agents and magnetic resonance imaging agents and so on. The perspectives of the foreseeable future and potential application of supramolecules as chemical drugs are also presented.

show abstract

Cyclodextrin/imatinib complexation: Binding mode and charge dependent stabilities

Cited by 59 publications

References 27 publications

Delivering drug-polymer complex via quick dissolving film: A step towards the development of an appropriate pediatric formulation

Delivering drug-polymer complex via quick dissolving film: A step towards the development of an appropriate pediatric formulation

Utility of cyclodextrins in the formulation of genistein

Review on supermolecules as chemical drugs

Contact Info

Product

Resources

About