Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Ghosh, Animesh; Biswas, Swati; Ghosh, Tanmoy

doi:10.4103/0975-1483.83759

Cited by 102 publications

(68 citation statements)

References 11 publications

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“…There are five main methods employed (Branchu et al, 1999;Chen et al, 2010;Ghosh et al, 2011;Peroche et al, 2005;Sapkal et al, 2007;Zhou et al, 2012) in previous studies to prepare the inclusion complex of cyclodextrin, including precipitation and co-precipitation method (or known as saturated water solution method), spray-drying process, grinding method, magnetic stirring method, and ultrasonic method. The two former methods were exempted at the beginning due to its inappropriateness for the drug in this study.…”

Section: Selected Methods and Optimizationmentioning

confidence: 99%

“…where S 0 is the intrinsic solubility of CAP at different temperatures in the absence of HP-b-CD (Ghosh et al, 2011). Change in Gibbs free energy (DG) is a criterion for ascertaining whether the reaction occurred spontaneously, which was calculated according to the equation (Pollard, 2010) DG ¼ ÀRT ln k.…”

Section: Characterization Of Inclusion Complexmentioning

confidence: 99%

“…But there are still some awaiting properties of b-CD that need to be improved, such as low aqueous solubility (18.5 g L À1 at 25 C), difficult in vivo metabolism, and nephrotoxicity (Del Valle, 2004) which is the main reason for its limited practical application. Hydroxypropyl-b-cyclodextrin (HP-b-CD), amorphism powder, a derivative of b-CD has several advantages including excellent absorption and bioavailability (Shulman et al, 2011), strong solubilizing power (Ghosh et al, 2011;Yuvaraja & Khanam, 2014), and stability (Miyake et al, 2000), less toxicity (de Araujo et al, 2008) and irritation of tissues (Vega et al, 2012), and well tolerated in animals (de Paula et al, 2011). Most importantly, it is the first b-CD derivative to get approval from United States Food and Drug Administration (USFDA) as an intravenous administration.…”

Section: Introductionmentioning

confidence: 99%

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Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation

Zhao

Sun

Shi

et al. 2015

Pharmaceutical Biology

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Context: Capsaicin (CAP) is an effective drug in the treatment of pain and cancer. However, its practical administration has been limited due to poor aqueous solubility and bioavailability, as well as strong gastrointestinal irritation. Objective: The objective of this study is to improve the solubility and oral bioavailability of CAP by reducing irritation via hydroxypropyl-b-cyclodextrin (HP-b-CD) inclusion complex formulation, in vitro and in vivo analysis. Materials and methods:The complex (CAP-HP-b-CD) was developed via the magnetic stirring method and characterized using ultraviolet (UV) absorption spectrometry, infrared radiation (IR) spectroscopy, and differential scanning calorimetry (DSC). Rats were treated with CAP (90 mg Â kg À1 ) or CAP-HP-b-CD (corresponding to 90 mg Â kg À1 CAP) by gavage, and all the plasma samples were analyzed with high performance liquid chromatography (HPLC). Results: The results of UV, IR, and DSC showed that an acceptable CAP-HP-b-CD (encapsulation efficiency, 75.83%; drug loading, 7.44%) was formulated. In vitro release study of CAP-HP-b-CD revealed that the cumulative release of CAP from HP-b-CD encapsulation was obviously enhanced (above 80% increases). Similarly, the in vivo pharmacokinetics parameters also increased, C max (from 737.94 to 1117.57 ng Â mL À1 ), AUC 0-(from 5285.9 to 7409.8 ng Â h Â mL À1 ) or relative bioavailability (139.38%). The gastric irritation bioassay further showed that the CAP-HP-b-CD was far better than free CAP. Discussion and conclusion: CAP exhibited significant aqueous solubility and oral bioavailability, as well as minimal irritation effect after forming inclusion complex with HP-b-CD. Therefore, these findings could provide an equally important alternative option for the clinical use of CAP. KeywordsHP-b-CD, in vitro release, irritation, oral bioavailability History

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Section: Selected Methods and Optimizationmentioning

confidence: 99%

Section: Characterization Of Inclusion Complexmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation

Zhao

Sun

Shi

et al. 2015

Pharmaceutical Biology

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“…The inclusion complexes can modify pharmacokinetic properties of guest molecules by fitting within the hydrophobic cavity of CDs [8,9]. Several NSAIDs have been complexed with CDs, which resulted in high solubility and dissolution rate, decreased side effects, reduced dose, improved bioavailability and stability, lesser gastric irritation and also enhanced the palatability of the active molecules [10][11][12][13].…”

Section: Fig 1: Structure Of Nimesulide [2]mentioning

confidence: 99%

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

2017

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Objective: The main objective of the research work was to optimize the water requirement/content used in kneading method for solid dispersion/inclusion complex formation between water insoluble drug and polymer.Methods: Nimesulide (model drug) and β-cyclodextrin were taken in a different ratio such as 1:1, 1:3 and 1:5 and, the mixture was triturated well for half hour. Water was incorporated to the mixture in different levels like 75%, 50%, 25% w/v in divided proportions and 0% (no water addition, but the mixture was triturated continuously). After each part of water addition, the mixture was triturated well for 10 min and dried using hot air over for 30 min at 50 °C and sieved using sieve no: 44. The complexes formed were subjected for various analytical characterization studies including solubility, particle size, the angle of repose, tapped density, Carr's index, fourier transform infrared spectrometry (FTIR), thermo gravimetric-differential thermal analysis (TG-TDA), x-ray diffraction (XRD) studies and in vitro dissolution studies. Results:The dissolution studies showed improvement in the release of nimesulide, which depended on the percentage level of water. The solubility of the sample was increased with increasing the concentration of the inclusion complex formed. Kneading method was proved to be a successful technique for formation of stable inclusion complex of nimesulide with β-cyclodextrin. All the formulations exhibited acceptable particle size and solubility in the range of 22.6±2 to 29±5 and 45±5 to 133±3.5 respectively. Conclusion:Nimesulide and β-cyclodextrin complex was successfully prepared and characterized for the drug-polymer stability and interactions. The result confirmed that the liquid content in the solid dispersion prepared by the kneading method played an important role in the dissolution of the poorly soluble drug.

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“…Kneading is an encapsulation method in which a homogenous paste of the excipient materials is prepared in a mixer or mortar with the addition of small quantities of water. This step is followed by the gradual addition of the guest material to the paste, with continuous kneading to attain a suitable consistency, followed by drying of the paste (Ghosh et al, 2011). Kneading is a typical processing step in the preparation of host-guest complexes containing CDs, and many elementary studies have described such methods for encapsulating the oils of flavoring agents.…”

mentioning

confidence: 99%

Encapsulation of Retinyl Palmitate with a Mixture of Cyclodextrins and Maltodextrins by the Kneading Method

Koeda

Wada²,

Neoh

et al. 2014

FSTR

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In this study, encapsulation of retinyl palmitate using the kneading method was investigated. The wall materials Keywords: retinyl palmitate, cyclodextrin, maltodextrin, dextrose equivalent value, encapsulation IntroductionRetinoids are natural and synthetic derivatives of vitamin A.The most common forms of vitamin A precursors present in food are retinol and retinyl esters, which are stored as esters of fatty acids, predominantly as retinyl palmitate (ester of retinol and palmitate) (Tanumihardjo, 2011). Retinoids are essential nutrients for animals, affecting lipid and protein metabolism and endocrine system regulation. The chemical stability of retinoids, including retinyl palmitate, is strongly dependent on chemical and environmental factors such as the solvent, temperature, and oxygen availability (Ji and Seo, 1999). The protection offered by dietary vitamin A has been well established (Loveday and Singh, 2008;Sauvant et al., 2012); thus, enhancing retinoid stability by encapsulation has been extensively investigated. Gonnet et al. (2010) reviewed new trends in the encapsulation of liposoluble vitamins, including the encapsulation of vitamin A in the food industry. Encapsulation is an important method for protecting unstable compounds from damage due to oxidation and other degradative processes (Gonnet et al., 2010). The materials used for the encapsulation of vitamin A have been classified according to the stability of the constructs, which include solid particles, molecular complexes, emulsions, and liposomes (Sauvant et al., 2012). Molecular complexes of retinoids with cyclodextrins (CDs), proteins, and chitosan have been well studied. Retinoid-CD complexes are usually prepared by mixing the retinoids with CD in an aqueous solution (Gonnet et al., 2010;Lin et al., 2007), but this is not an easy procedure. A γ-CD/retinol complex with the required composition is commercially available (Regiert, 2009); however, its synthesis requires vigorous stirring for 72 h at 50℃ under a N 2 atmosphere (Moldenhauer et al., 1999). Lin et al. (2000) improved T. Koeda et al. 530 complex solubility and stability using a method for the preparation of a 2-hydroxypropyl-β-CD (HP-β-CD)/all-trans-retinoic acid complex that involved shaking the suspension under ambient temperature (24℃) for 8 d. Furthermore, Yoshida et al. (1999) tested the stability of retinol in emulsions and found that after 4 weeks at 50℃ in O/W, W/O, and O/W/O emulsions, the percentage of retinol remaining was 32.3%, 45.7%, and 56.9%, respectively.However, the emulsions contained only 0.1% retinol. Singh and Das (1998) studied the properties of retinol and retinyl palmitate intercalated in phosphatidylcholine liposomes. In general, spraydrying is commonly used to encapsulate food ingredients with solid particles (Gharsallaoui et al., 2007), and many encapsulated powders are manufactured by emulsification of substrates with surfactants in maltodextrin (MD) solutions and spray-drying the resulting mixtures. The efficacies of three different processes, n...

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Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Cited by 102 publications

References 11 publications

Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation

Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

Encapsulation of Retinyl Palmitate with a Mixture of Cyclodextrins and Maltodextrins by the Kneading Method

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