In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation

Sinha, Vivek Ranjan; Amita,; Goel, Honey

doi:10.3797/scipharm.0909-08

Cited by 13 publications

(6 citation statements)

References 7 publications

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“…Also, the most crucial and important pharmacokinetic parameter t 1/2 (73.78 min) was prolonged (2.17 folds greater) for kneaded complex than the pure drug (34 min). These results were similar to the work done by Sinha and Goel 29 . Also, CD-drug complexes could increase the oral bioavailability of drugs by improving their solubility and through liposolubility.…”

Section: Pharmacokinetics and In-vivo Plasma Studiessupporting

confidence: 94%

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gidwani

Vyas

2015

Drug Development and Industrial Pharmacy

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The objective of the present work was to investigate the inclusion behavior of bendamustine (BM) with β-cyclodextrin and its hydrophilic derivatives (HP-β-CD and Epi-β-CD) for the enhancement of aqueous solubility, dissolution and bioavailability. The supramolecular binary complexes were prepared by three different methods, viz. physical mixture (PM), kneading (KND) and co-evaporation (COE). Phase-solubility study revealed the higher solubilizing and complexing ability of polymerized cyclodextrin (Ks = 645 M(-1)) than parent cyclodextrin (Ks = 43 M(-1)) and chemically derived cyclodextrin (Ks = 100 M(-1)). Meanwhile, the solubility of BM was significantly enhanced in phosphate buffer of pH 6.8, which was 24.5 folds greater compared with the phosphate buffer pH 4.5 and four times greater than aqueous medium. The dissolution efficiency was found to be highest for BM: Epi-β-CD complex (87%) compared to BM: HP-β-CD complex (84%), BM: β-CD (79%) and pure drug (20%). In-vivo pharmacokinetic study revealed that the bioavailability of BM was enhanced 2.55 times on complexation with Epi-β-CD using KND method. The t1/2 of BM was increased from 34.2 min to approximately 75.7 min, allowing the absorption for longer time. The order of increase in solubility, dissolution and bioavailability of BM was KND > COE > PM > pure drug. Thus, the strategy of host-guest inclusion was very effective and could be successfully used in the development of suitable pharmaceutical dosage form with enhanced therapeutic activity.

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Section: Pharmacokinetics and In-vivo Plasma Studiessupporting

confidence: 94%

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gidwani

Vyas

2015

Drug Development and Industrial Pharmacy

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“…The percent change in paw swelling (% edema) compared to baseline measurement was taken as the criterion of comparison [ 31 ]. The inhibition % of the induced edema was used as an indicator to measure the anti-inflammatory effect in comparison with the control [ 39 ]: % edema = (test paw thickness − initial paw thickness)/(initial paw thickness) × 100 [ 40 ] and % inhibition of inflammation = [(control % edema − test % edema) × 100]/(control % edema) [ 40 , 41 ].…”

Section: Methodsmentioning

confidence: 99%

Effect of Polymers on the Physicochemical Properties and Biological Performance of Fenoprofen Calcium Dihydrate-Triacetyl-β-Cyclodextrin Complex

2017

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Background: Fenoprofen calcium dehydrate (FCD) is counted as a non-steroidal, anti-inflammatory, anti-arthritic drug. FCD is slightly water soluble. It is indicated for mild pain relief, where the suggested dosage is 200 mg orally every 4 to 6 h. Aim: Reduce dissolution efficiency, reach an extended therapeutic effect and reduce the frequency of the drug side effects. Method: Combination of the co-evaporated drug:triacetyl-β-cyclodextrin complex prepared in a ratio of 1:3 and either of two polymers—hydroxylpropylmethyl cellulose (HPMC) or ethyl cellulose (EC)—in the same formulation. In vitro dissolution studies were carried in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids, by using the USP dissolution tester (rotating paddle apparatus). The FCD in vitro release from EC/drug complex was markedly retarded. Interaction between fenoprofen, TA-β-CD, EC, HPMC in the solid state were confirmed by FT-IR, DSC, XRD and SEM. In vivo studies assessed the anti-inflammatory and analgesic activities and the results were compared with the market product Nalfosab® Capsules. Results: Remarkable inhibition of inflammation and nociception after 24 h was attained for EC/drug complex. Conclusions: EC/drug complex has a sustained effect due to high remaining amount after elapsing with remarkable inhibition of inflammation.

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“…These drug/host complexes may alter drug metabolism route, biodistribution, and tubular reabsorption, and thereby the bioavailability of drugs can be changed. In particular, myricetin [90], isotretinoin [91], benznidazole [92], and etodolac exhibit 9.4-, 4.7-, 3.6-, and 2.5-fold increases in bioavailability upon addition of drug/CD derivative complexes for their oral administration [93]. As well as, the CDs are ultimately digested by bacteria in the gastrointestinal tract or colon to monosaccharides or gases including carbon dioxide, hydrogen, and methane [94].…”

Section: Oligosaccharidesmentioning

confidence: 99%

Supramolecular Complexation of Carbohydrates for the Bioavailability Enhancement of Poorly Soluble Drugs

Cho

Jung

2015

Molecules

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Abstract:In this review, a comprehensive overview of advances in the supramolecular complexes of carbohydrates and poorly soluble drugs is presented. Through the complexation process, poorly soluble drugs could be efficiently delivered to their desired destinations. Carbohydrates, the most abundant biomolecules, have diverse physicochemical properties owing to their inherent three-dimensional structures, hydrogen bonding, and molecular recognition abilities. In this regard, oligosaccharides and their derivatives have been utilized for the bioavailability enhancement of hydrophobic drugs via increasing the solubility or stability. By extension, polysaccharides and their derivatives can form self-assembled architectures with poorly soluble drugs and have shown increased bioavailability in terms of the sustained or controlled drug release. These supramolecular systems using carbohydrate will be developed consistently in the field of pharmaceutical and medical application.

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In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation

Cited by 13 publications

References 7 publications

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Effect of Polymers on the Physicochemical Properties and Biological Performance of Fenoprofen Calcium Dihydrate-Triacetyl-β-Cyclodextrin Complex

Supramolecular Complexation of Carbohydrates for the Bioavailability Enhancement of Poorly Soluble Drugs

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