Diclofenac-β-cyclodextrin binary systems: Physicochemical characterization and in vitro dissolution and diffusion studies

Manca, Maria Letizia; Zaru, Marco; Ennas, Guido; Valenti, Donatella; Sinico, Chiara; Loy, Giuseppe; Fadda, Anna Maria

doi:10.1208/pt060358

Cited by 56 publications

(20 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Enhancement of API release increases absorption by improving bioavailability. 40,41 This was confirmed in the present studies, which showed that K/ b-CD had a higher efficiency than the noncomplexed API. The anti-inflammatory and analgesic effects of the complex were significantly higher and occurred faster, even at low dose rates (15 mg/m 2 body surface), in both types of experimental inflammation.…”

Section: Discussionsupporting

confidence: 87%

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

Grecu¹,

Nastasa²,

Ilie

et al. 2013

Lab Anim

View full text Add to dashboard Cite

Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) can lead to adverse effects such as gastrointestinal distress. The complexation of different groups of active substances with b-cyclodextrin (b-CD) has drawn considerable interest over recent years. The purpose of this study was to analyze the ketoprofen/b-cyclodextrin (K/b-CD) conjugate complex as well as to assess its anti-inflammatory effect after oral administration (doses of 30 mg/m 2 and 15 mg/m 2 of body surface), compared with ketoprofen. The studies were done on two models of experimentally-induced acute inflammation in rats (n ¼ 48, 6/group), by means of intraplantar administration of a 10% aqueous kaolin suspension and intraperitoneal administration of a 1% sodium thioglycolate solution. The dynamics of the acute inflammatory process and the anti-inflammatory effects were monitored using plethysmometric determinations after 3, 6, 9, 12, 24 and 48 h (plantar inflammation), and the absorbance of the exudates (spectrophotometrically read) and nucleated cell counts after 24 h (peritoneal inflammation). The coupling of ketoprofen with b-CD resulted in increased solubility (100% in 60 min) of the newly-formed product, which further resulted in a higher bioavailability compared with ketoprofen (<40% in 120 min). In both models of experimentally-induced inflammation, the K/b-CD complex had a higher anti-inflammatory activity than ketoprofen.

show abstract

Section: Discussionsupporting

confidence: 87%

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

Grecu¹,

Nastasa²,

Ilie

et al. 2013

Lab Anim

View full text Add to dashboard Cite

show abstract

“…[1][2][3] They have been widely used as complexing agents to modify drug solubility or improve drug stability, and bioavailability, by means of drug inclusion into the hydrophobic cavity of cyclodextrin. CDs are thus offering new hope to formulation scientists in their efforts to develop an effective drug delivery system.…”

Section: Introductionmentioning

confidence: 99%

Carvedilol-?-cyclodextrin Systems: Preparation, Characterization and in vitro Evaluation

Sharma¹,

Jain

2013

Dhaka Univ. J. Pharm. Sci

View full text Add to dashboard Cite

ABSTRACT:The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a complex with β-cyclodextrin. Phase solubility diagrams revealed increase in solubility of the drug upon cyclodextrin addition, showing A N type curve. Complexation of carvedilol was carried out with β-cyclodextrin by physical mixing, kneading and co-precipitation method. The prepared complexes and physical mixture were characterized by Fourier transform infra red spectroscopy, differential scanning calorimetry, powder X-ray diffractometry and inclusion efficiency. It was also observed that the complexes exhibit higher dissolution rates than the pure drug and physical mixture. Among all carvedilol-cyclodextrin complexes, inclusion complex (1:5) prepared by co-precipitation method showed better release.

show abstract

“…In an aqueous solution, the complexes get readily dissociated, and the free drug molecules are in relatively rapid dynamic equilibrium with drug molecules bound within the CD cavity. [45][46][47] These non-covalent complexes show new physicochemical characteristics when compared with the guest molecules, including better stability, higher aqueous solubility, increased bioavailability and fewer undesirable side effects. [48] Therefore, if it is possible to form statin-CD inclusion complexes and control their solubility, it should be possible to control their drug-release properties.…”

Section: Cyclodextrin Inclusion Systemmentioning

confidence: 99%

Statins therapy: a review on conventional and novel formulation approaches

Tiwari

Pathak

2011

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Background and objective High levels of cholesterol lead to atherosclerosis, a factor predisposing to the development of coronary artery disease. Statin drugs, i.e. HMG-CoA reductase inhibitors, have been known since the end of the last century for their benefits against cardio-and cerebrovascular diseases and are widely used clinically. This review aims at compiling the research inputs being made for developing therapeutically efficacious dosage forms that have the potential to surmount the limitations of conventional dosage forms of statins. Key findings Statin drugs can reduce the endogenous synthesis of cholesterol and prevent the onset and development of atherosclerosis, and are therefore used as an effective treatment against primary hypercholesterolemia. At present, statin drugs are most often administered orally, on a daily basis. After administration, the bioavailability and the general circulation of statin drugs is fairly low due to the first-pass metabolism in the liver and clearance by the digestive system. Extensive pharmaceutical research in understanding the causes of low oral bioavailability has led to the development of novel technologies to address these challenges. Summary These technologies vary from conventional dosage forms to nanoparticulate drug-delivery systems, and have the potential to cause improvements in bioavailability and consequently therapeutic efficacy.

show abstract

Diclofenac-β-cyclodextrin binary systems: Physicochemical characterization and in vitro dissolution and diffusion studies

Cited by 56 publications

References 26 publications

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

Carvedilol-?-cyclodextrin Systems: Preparation, Characterization and in vitro Evaluation

Statins therapy: a review on conventional and novel formulation approaches

Contact Info

Product

Resources

About