Characterization and in vivo evaluation of lacidipine inclusion complexes with β-cyclodextrin and its derivatives

Darekar, T.; Aithal, K. S.; Shirodkar, Rupesh Kalidas; Kumar, Lalit; Attari, Zenab; Lewis, Shaila

doi:10.1007/s10847-016-0600-9

Cited by 17 publications

(11 citation statements)

References 34 publications

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“…Some changes observed in the O-H stretching vibration (absorption peak at 3460 cm −1 ), could allow probing the alteration of the H-bonded environments upon complexation. The O-H bending vibrations of CH 2 OH and C-H stretching vibrations of HPβCD got distorted due to the inclusion of guests to the host cavity, as has been reported in other researches (Darekar et al 2016).…”

Section: Ft-ir Characterization Of Hpβcd-tropane Alkaloids Inclusion Complexsupporting

confidence: 70%

“…2 FT-IR absorption spectra of tropane alkaloids, hydroxypropyl β-CD (HPβCD), and inclusion complex, in the range 4000-400 cm -1 (a) and 2000-400 cm -1 (b) FT-IR spectrum of alkaloids tropane is characterized by typical absorption peaks for the stretching vibrations of various functional groups; 3700-3000 cm −1 (O-H alcohol, N-H amine), 3104 cm −1 (aromatic C-H), 1738 cm −1 (C = O ester), 1650 cm −1 (N-H bending), 1496 cm −1 (C = C aromatic), 1600-1300 cm −1 (C-H bending alkane), 1200 (C-O ester), 1050 cm −1 (C-O primary alcohol), 900-700 cm −1 (C-H aromatic bending vibrations) (Baranska and Schulz 2009;Christen et al 2009). FT-IR spectrum of HPβCD showed the main peaks related to the stretching vibrations of the functional groups: 3460 cm −1 (O-H), 3000 cm −1 (C-H), 1160 cm −1 (O-H of CHOH) 1050 cm −1 (C-O-C ether linkage) 1021 cm −1 (C-O of CH 2 OH) 800-650 cm −1 (C-H bending vibrations) (Darekar et al 2016;Gao, 2019a;Su et al 2012).…”

Section: Ft-ir Characterization Of Hpβcd-tropane Alkaloids Inclusion Complexmentioning

confidence: 99%

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Analytical and in silico study of the inclusion complexes between tropane alkaloids atropine and scopolamine with cyclodextrins

et al. 2021

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Datura stramonium L. (Solanaceae) possesses a rich tropane alkaloids (TAs) spectrum. The plant contains, in particular, the allelopathic compounds scopolamine and atropine, which are poorly soluble in water, thus limiting their use in agrochemical formulations as biocidal and deterrent agents against herbivore insects. The efficacy of the hydrophobic TAs extracts could be increased with the improvement of their dissolution/leaching properties. This is important for improving screening and test performance and for elucidating the activity of environmentally friendly agricultural approaches, with new perspectives for the production and use of those biodegradable insecticidal products. The present study explores the aspects of atropine and scopolamine complexation with cyclodextrin (CDs) through FT-IR and UV–Vis spectroscopies. In addition, the structures of the inclusion complex of atropine, scopolamine and β-CD have been investigated by molecular modeling techniques. The results obtained indicate that β-CDs are a promising carriers for improving the properties of TAs, therefore increasing their application potential in agrochemical formulations. Graphic abstract

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Section: Ft-ir Characterization Of Hpβcd-tropane Alkaloids Inclusion Complexsupporting

confidence: 70%

Section: Ft-ir Characterization Of Hpβcd-tropane Alkaloids Inclusion Complexmentioning

confidence: 99%

Analytical and in silico study of the inclusion complexes between tropane alkaloids atropine and scopolamine with cyclodextrins

et al. 2021

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“…LCDP suffers from low oral bioavailability about 10% (range 3–59%) due to extensive hepatic first-pass metabolism by cytochrome P450 3A4 (CYP3A4). In addition, LCDP is a highly lipophilic BCS class II drug with poor aqueous solubility which contributes to its limited bioavailability (Basalious et al., 2010 ; Gannu et al., 2010 ; Wu et al., 2015 ; Zhao et al., 2015 ; Darekar et al., 2016 ).…”

Section: Introductionmentioning

confidence: 99%

Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study

2017

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This study aims at preparing and optimizing lacidipine (LCDP) polymeric micelles using thin film hydration technique in order to overcome LCDP solubility-limited oral bioavailability. A two-factor three-level central composite face-centered design (CCFD) was employed to optimize the formulation variables to obtain LCDP polymeric micelles of high entrapment efficiency and small and uniform particle size (PS). Formulation variables were: Pluronic to drug ratio (A) and Pluronic P123 percentage (B). LCDP polymeric micelles were assessed for entrapment efficiency (EE%), PS and polydispersity index (PDI). The formula with the highest desirability (0.959) was chosen as the optimized formula. The values of the formulation variables (A and B) in the optimized polymeric micelles formula were 45% and 80%, respectively. Optimum LCDP polymeric micelles had entrapment efficiency of 99.23%, PS of 21.08 nm and PDI of 0.11. Optimum LCDP polymeric micelles formula was physically characterized using transmission electron microscopy. LCDP polymeric micelles showed saturation solubility approximately 450 times that of raw LCDP in addition to significantly enhanced dissolution rate. Bioavailability study of optimum LCDP polymeric micelles formula in rabbits revealed a 6.85-fold increase in LCDP bioavailability compared to LCDP oral suspension.

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“…Dissolution studies were carried out using 500 ml of purified water with 1% w/v polysorbate 20, at 50 rpm and at temperature of 37±0.5 C˚. 10 ml aliquots were withdrawn at suitable time interval (5,10,15,20,25,30,35, 40 and 45 min), filtered through syringe filter 0.45µm and diluted as per need and replaced with fresh medium.…”

Section: In Vitro Drug Dissolution Testmentioning

confidence: 99%

“…The chemical structure of lacidipine was shown in fig. (1) Fig. 1: Chemical structure of lacidipine [10] In the present study, a poorly soluble calcium channel blocker lacidipine were prepared as liquisolid compacts using water-miscible non-volatile solvents to enhance solubility and the dissolution rate with compare the in vitro drug release profile of formulated liquisolid tablets with the prepared direct compressed tablet.…”

Section: Introductionmentioning

confidence: 99%

Preparation and in Vitro Evaluation of Lacidipine Oral Liquid Solid Tablet as an Approach of Solubility and Dissolution Rate Enhancement

Rajab

2018

Int J App Pharm

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Objective: The aim of the present study was to prepare a new liquid-solid tablet to enhance the dissolution and bioavailability of a poor water soluble calcium channel blocker lacidipine.Methods: Firstly, solubility study of lacidipine in different media of water-miscible non-volatile solvents as tween 20, tween 80, propylene glycol, liquid paraffin, PEG200, PEG400, and PEG600 was investigated to select the most suitable solvent. A mathematical model was applied to calculate the appropriate amount of carrier and coating material.Four liquid-solid tablets of 6 mg lacidipine were prepared by dissolving the drug in the previously chosen water miscible non-volatile solvents, then a binary mixture of the carrier (Avicel PH 102) and coating material (Aerosil 200) at a ratio of 45:1 was used in all preparation since it gave the optimal flow property. Croscarmellose and magnesium stearate were incorporated in all prepared formulas as super disintegrant and lubricant respectively. On the other hand, directly compressed lacidipine tablet of the same previous composition without the addition of any non-volatile solvent was prepared for comparism study. Both characterizations of powder mixture and post-compression tablet evaluations were done. Differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were investigated for the pure drug, physical mixture, and selected liquid-solid tablet to exclude any drug-excipients interaction. Results:The obtained results indicated that PEG 200 was the most suitable solvent with lacidipine solubility of 2.81 mg/ml. Flowability of all the prepared formulas was found to be within the specification limits. The liquid-solid tablet formula with PEG 200 at 10% w/w lacidipine was the most suitable one in the term of disintegration time (21±0.2 second), 100% of drug release within 10 min, and with accepted other tablet properties.DSC thermograms for both physical mixture of selected liquisolid system and its tablets illustrated the formation of lacidipine amorphous solid solution. The absence of chemical interaction between drug and other formula components was confirmed by remaining all characteristic peaks of lacidipine in all investigated FTIR spectra. Conclusion:Liquid-solid tablet was considered as a promising system to enhance solubility and dissolution rate of poor-water soluble lacidipine.

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Characterization and in vivo evaluation of lacidipine inclusion complexes with β-cyclodextrin and its derivatives

Cited by 17 publications

References 34 publications

Analytical and in silico study of the inclusion complexes between tropane alkaloids atropine and scopolamine with cyclodextrins

Analytical and in silico study of the inclusion complexes between tropane alkaloids atropine and scopolamine with cyclodextrins

Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study

Preparation and in Vitro Evaluation of Lacidipine Oral Liquid Solid Tablet as an Approach of Solubility and Dissolution Rate Enhancement

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