Improved oral delivery of clonazepam through liquisolid powder compact formulations: In-vitro and ex-vivo characterization

Sanka, Krishna; Poienti, Sravanthi; Mohd, Abdul Bari; Diwan, Prakash V.

doi:10.1016/j.powtec.2014.02.026

Cited by 36 publications

(16 citation statements)

References 39 publications

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“…This value is considerably lower in comparison to liquisolid tablets, which showed an 80% release of drug during the first five minutes of testing. The same enhanced release profile has already been proved in several studies dealing with liquisolid systems, such as those of liquisolid compacts containing clonazepam [ 43 ], candesartan cilexetil [ 44 ], and griseofulvin [ 35 ]. The enhanced release could be caused by the presence of a nonvolatile liquid vehicle which improved the wettability of the compacts and hence their disintegration time and by the presence of the drug in its dissolved form without the need to dissolve it in the dissolution medium [ 14 ].…”

Section: Resultsmentioning

confidence: 53%

Modern Evaluation of Liquisolid Systems with Varying Amounts of Liquid Phase Prepared Using Two Different Methods

Vraníková

Gajdziok

Vetchý

2015

BioMed Research International

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Liquisolid systems are an innovative dosage form used for enhancing dissolution rate and improving in vivo bioavailability of poorly soluble drugs. These formulations require specific evaluation methods for their quality assurance (e.g., evaluation of angle of slide, contact angle, or water absorption ratio). The presented study is focused on the preparation, modern in vitro testing, and evaluation of differences of liquisolid systems containing varying amounts of a drug in liquid state (polyethylene glycol 400 solution of rosuvastatin) in relation to an aluminometasilicate carrier (Neusilin US2). Liquisolid powders used for the formulation of final tablets were prepared using two different methods: simple blending and spraying of drug solution onto a carrier in fluid bed equipment. The obtained results imply that the amount of liquid phase in relation to carrier material had an effect on the hardness, friability, and disintegration of tablets, as well as their height. The use of spraying technique enhanced flow properties of the prepared mixtures, increased hardness values, decreased friability, and improved homogeneity of the final dosage form.

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Section: Resultsmentioning

confidence: 53%

Modern Evaluation of Liquisolid Systems with Varying Amounts of Liquid Phase Prepared Using Two Different Methods

Vraníková

Gajdziok

Vetchý

2015

BioMed Research International

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“…Thus, bioavailability is predicted to be increased if most of the drug is absorbed from the gastric cavity rather than from the intestine. To investigate whether formulation in an LT can enhance permeation of curcumin as shown for other drugs 53 , an ex vivo permeation study was performed. Since the gastric transit time is 2 h, the study was designed to estimate drug permeation within 2 h. The percent cumulative drug permeated (CDP) was found to be 89.2% with an r 2 0–20min value (coefficient of regression ranges from 0 to 20 min) of 0.9854 in the initial phase followed by r 2 20–120min (coefficient of regression ranges from 20 to 120 min) of 0.8445 in the later phase.…”

Section: Resultsmentioning

confidence: 99%

Effect of hydrogen bond formation/replacement on solubility characteristics, gastric permeation and pharmacokinetics of curcumin by application of powder solution technology

Sharma

Pathak

2016

Acta Pharmaceutica Sinica B

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The present research aimed to improve the dissolution rate and bioavailability of curcumin using the potential of liquisolid technology. Twelve drug-loaded liquisolid systems (LS-1 to LS-12) were prepared using different vehicles (PEG 200, PEG 400 and Tween 80) and curcumin concentrations in vehicle (40%, 50%, 60% and 70%, w/w). The carrier [microcrystalline cellulose (MCC) PH102] to coat (Aerosil®) ratio was 20 in all formulations. The systems were screened for pre-compression properties before being compressed to liquisolid tablets (LT-1 to LT-12). Post compression tests and in vitro dissolution of LTs were conducted and the results compared with those obtained for a directly compressed tablet (DCT) made of curcumin, MCC PH102 and Aerosil®. LTs exhibited higher cumulative drug release (CDR) than the DCT and the optimum formulation, LT-9 (made using Tween 80), was studied by powder XRD, DSC, SEM and FTIR. Ex-vivo permeation of curcumin from LT-9 through goat gastrointestinal mucosa was significantly (P<0.05) enhanced and its oral bioavailability was increased 18.6-fold in New Zealand rabbits. In vitro cytotoxicity (IC50) of LT-9 towards NCL 87 cancer cells was 40.2 µmol/L substantiating its anticancer efficacy. Accelerated stability studies revealed insignificant effects of temperature and humidity on LT-9. In summary, solubility enhancement of curcumin in LTs produced significant improvements in its permeation and bioavailability.

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“…XRD of pure drug candesartan cilexetil showed sharp diffraction peak at two-theta values 9.8, 17.2 and 23.2, while liquisolid powder showed no characteristic peak, thus indicated conversion of drug from crystalline to amorphous form ( Figure 5). 23 Absence of drug crystallinity peak assured solubilization of drug in liquid vehicle (Transcutol HP) that was further absorbed and adsorbed onto carrier material (Neusilin) and coat material (Aerosil 200). Figure 6 shows IR spectra of percentage transmission (%T) versus wave number of pure candesartan cilexetil and liquisolid compacts.…”

Section: Xrd Studymentioning

confidence: 99%

Liquisolid Compact Tablet of Candesartan Cilexetil with Enhanced Solubility using Neusilin US2, Aerosil 200 and Transcutol HP

Argade¹,

Patole²,

Pandit³

2019

IJPER

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Objective: An attempt was made to enhance solubility, dissolution and intestinal permeability of drug candesartan cilexetil by liquisolid technology. Methods: Liquisolid tablet was formulated using non-volatile solvent Transcutol HP, carrier material Neusilin US2 and coating material Aerosil 200. Appropriate quantities of excipients were calculated with the help of mathematical model to get liquisolid powder. A 3 2 full-factorial design was used further to optimize liquisolid powder. Results: DSC, XRD and SEM studies revealed absence of crystalline nature of drug in liquisolid powder. Liquisolid powder was further compressed into tablet and subjected to various evaluation tests such as in-vitro drug release and ex-vivo intestinal permeation study. Conclusion: Liquisolid technology was found to be promising due to enhance solubility, dissolution and permeation of candesartan cilexetil by 19.75, 3.09 and 2.4-fold, respectively.

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Improved oral delivery of clonazepam through liquisolid powder compact formulations: In-vitro and ex-vivo characterization

Cited by 36 publications

References 39 publications

Modern Evaluation of Liquisolid Systems with Varying Amounts of Liquid Phase Prepared Using Two Different Methods

Modern Evaluation of Liquisolid Systems with Varying Amounts of Liquid Phase Prepared Using Two Different Methods

Effect of hydrogen bond formation/replacement on solubility characteristics, gastric permeation and pharmacokinetics of curcumin by application of powder solution technology

Liquisolid Compact Tablet of Candesartan Cilexetil with Enhanced Solubility using Neusilin US2, Aerosil 200 and Transcutol HP

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