Design and Evaluation of Cyclodextrin-Based Drug Formulation

Uekama, Kaneto

doi:10.1248/cpb.52.900

Cited by 320 publications

(142 citation statements)

References 157 publications

Supporting

Mentioning

137

Contrasting

Unclassified

Order By: Relevance

“…This solution was autoclaved at 120 ° C for half an hour to activate water soluble polymer through heating for enhanced drug solubilization [27,28] and then grounded for 6 h. An appropriate quantity of water was added to the mixture to maintain the desired consistency. The pastes were dried in an oven at 45-50 ° C for 24 h. The dried complexes were pulverized and then sieved through 120 #.…”

Section: Preparation Of Complexesmentioning

confidence: 99%

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

Arora¹,

Singh²,

Chadha

2017

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

Objective: The present work was aimed to study the effect of the ternary component on complexation efficiency of cyclodextrins towards telmisartan which is a poorly soluble anti-hypertensive agent. Methods:The elucidation of inclusion complexation of telmisartan (TEL) with hydroxypropyl-β-cyclodextrin (HP-β-CD) in the presence and absence of tween 80 was done by investigating their interactions in solid and solution state. The solid state characterization was performed using differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD) fourier transform infra-red spectroscopy (FTIR) studies. The host guest stoichiometry was confirmed in solution state by proton nuclear magnetic resonance ( 1 HNMR) and solution calorimetry studies. The improvement in solubility was evaluated through dissolution studies, which was further confirmed by in vivo studies. Results:In solution state, the phase solubility studies indicated 1:1 stoichiometry between TEL and HP-β-CD both in presence and absence of tween 80. The NMR and molecular modelling studies indicated the insertion of N-methyl benzimidazole and biphenyl carboxylate regions of TEL into HP-β-CD cavity suggesting the coexistence of two 1:1 complexes in equilibrium with each other. The stability constants, K1 (imidazole region of TEL-CD) and K2 (biphenyl acetic acid region of TEL-CD), were enhanced in the presence of tween 80 as evident by the higher value of stability constants. Efficacy of ternary complex was established by a significant decrease in the systolic blood pressure of deoxycorticosterone acetate (DOCA) induced hypertensive rats. Conclusion:It can be concluded that solubility of TEL was increased by encapsulation with HP-β-CD. Tween 80 further increased the complexation efficiency and decreased the bulk of cyclodextrin.

show abstract

Section: Preparation Of Complexesmentioning

confidence: 99%

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

Arora¹,

Singh²,

Chadha

2017

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

show abstract

“…Cyclodextrins are amphiphilic oligosaccharides that increase drug stability and absorption [140] ; after oral administration, they are split up into small saccharides in the colon, leaving Ang-(1-7) to be absorbed [18] . Chronic oral administration of Ang-(1-7)-CyD in isoproterenol-treated rats increases plasma Ang-(1-7) levels, with attenuation of myocardial infarction associated with cardioprotective effects [141] .…”

Section: New Targets For Hypertension Treatmentmentioning

confidence: 99%

Renin-angiotensin system in the kidney: What is new?

Ferrão

Lara

Lowe

2014

WJN

View full text Add to dashboard Cite

The renin-angiotensin system (RAS) has been known for more than a century as a cascade that regulates body fluid balance and blood pressure. Angiotensin Ⅱ (Ang Ⅱ) has many functions in different tissues; however it is on the kidney that this peptide exerts its main functions. New enzymes, alternative routes for Ang Ⅱ formation or even active Ang Ⅱ-derived peptides have now been described acting on Ang Ⅱ AT1 or AT2 receptors, or in receptors which have recently been cloned, such as Mas and AT4. Another interesting observation was that old members of the RAS, such as angiotensin converting enzyme (ACE), renin and prorenin, well known by its enzymatic activity, can also activate intracellular signaling pathways, acting as an outside-in signal transduction molecule or on the renin/(Pro)renin receptor. Moreover, the endocrine RAS, now is also known to have paracrine, autocrine and intracrine action on different tissues, expressing necessary components for local Ang Ⅱ formation. This in situ formation, especially in the kidney, increases Ang Ⅱ levels to regulate blood pressure and renal functions. These discoveries, such as the ACE2/Ang-(1-7)/Mas axis and its antangonistic effect rather than classical deleterious Ang Ⅱ effects, improves the development of new drugs for treating hypertension and cardiovascular diseases. Key words: Renin-angiotensin system; Angiotensin Ⅱ; Kidney; Hypertension treatment; Receptor Core tip: Activation of the angiotensin converting enzyme (ACE)/ Angiotensin Ⅱ (Ang Ⅱ)/AT1 axis leads to vasoconstriction, anti-diuresis, anti-natriuresis, release of aldosterone and anti-diuretic hormone, which can result in hypertension, renal and cardiovascular diseases. Inhibition of renin and ACE or blocking AT1 receptor is the most used therapies for heart failure and hypertension. Nevertheless, the discovery of local Ang Ⅱ synthesis, new Ang Ⅱ metabolites, receptors and axis of this system, makes possible the development of new drugs and strategies for renal and cardiovascular diseases treatment, such as activation of ACE2/Ang-(1-7)/ Mas axis, which presents opposite effects of AT1 activation by Ang Ⅱ.

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

Design and Evaluation of Cyclodextrin-Based Drug Formulation

Cited by 320 publications

References 157 publications

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

Renin-angiotensin system in the kidney: What is new?

Statins therapy: a review on conventional and novel formulation approaches

Contact Info

Product

Resources

About