A systematic physicochemical investigation on solubilization and in vitro release of poorly water soluble oxcarbazepine drug in pluronic micelles

2016 ◽  
Vol 504 ◽  
pp. 479-488 ◽  
Author(s):  
Pankaj Singla ◽  
Shruti Chabba ◽  
Rakesh Kumar Mahajan
Keyword(s):  
In Vitro Release ◽  
Water Soluble ◽  
Physicochemical Investigation ◽  
Poorly Water Soluble ◽  
Vitro Release

scholarly journals Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability

2020 ◽  
Vol 88 (4) ◽  
pp. 52
Author(s):  
Mona Qushawy ◽  
Ali Nasr ◽  
Shady Swidan ◽  
Yasmin Mortagi
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Production Yield ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Drug Content ◽  
Vitro Release

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial design. The prepared formulations were evaluated for production yield, drug content, micromeritic properties, thermal analysis, in-vitro release, and in-vivo hypoglycemic effect. All prepared formulations showed high production yield ranged from 98.4 ± 2.8 to 99.8 ± 2.2% and high drug content in the range of 97.2 ± 3.2 to 99.6 ± 2.1%. The micromeritic properties revealed that all prepared glimepiride formulations showed good flowability. The differential scanning calorimetry study revealed the presence of the drug in the more soluble amorphous form. In accordance with the results of in vitro release study, it was found that the solubility of glimepiride was increased by increasing the drug carrier ratio, compared with the pure form of the drug. It was found that F9 showed a high and rapid reduction in blood glucose levels in diabetic rats, which indicated the success of a solid dispersion technique in improving the solubility and hence the bioavailability of glimepiride.

scholarly journals Study on the influence of technological factors on drug loading of poorly water-soluble drug on MCM-41 mesoporous carrier

Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 351-356
Author(s):  
Teodora Popova ◽  
Christina Voycheva ◽  
Borislav Tzankov
Keyword(s):  
Loading Rate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Water Soluble ◽  
Technological Factors ◽  
Loading Process ◽  
Water Soluble Drug ◽  
Vitro Release ◽  
Mcm 41

The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained.

Inclusion Complex Formation of Water- Soluble Drug, Captopril, and Peracetylated-β-Cyclodextrin in Supercritical CO2 for Controlled Release Applications

2007 ◽  
Vol 342-343 ◽  
pp. 489-492 ◽  
Author(s):  
Hullathy Subban Ganapathy ◽  
Min Hee Woo ◽  
Yeong Soon Gal ◽  
Kwon Taek Lim
Keyword(s):  
Carbon Dioxide ◽  
Inclusion Complex ◽  
In Vitro Release ◽  
Water Soluble ◽  
Inclusion Complex Formation ◽  
Hydrophobic Properties ◽  
Water Soluble Drug ◽  
Xrd Studies ◽  
Vitro Release

The inclusion complex of CO2-soluble peracetylated-β-cyclodextrin (PAc-β- CD), heptakis(2,3,6-tri-O-acetyl)-β-cyclodextrin, and highly water-soluble drug captopril, was prepared by a chemical solvent-free method using supercritical carbon dioxide. The captopril-PAc-β-CD inclusion complex was further confirmed by DSC and XRD studies. In- vitro release of captopril from an oily suspension confirmed that the dissolution rate of captopril was much retarded from the inclusion complex as a result of the hydrophobic properties of PAc-β-CD.

Hydrophobically Modified Amphiphilic Cylodextrins as Novel Carriers for Controlled Delivery of Water-Soluble Drugs

2007 ◽  
Vol 342-343 ◽  
pp. 493-496 ◽  
Author(s):  
Hullathy Subban Ganapathy ◽  
Min Young Lee ◽  
Min Hee Woo ◽  
Yeong Tae Jeong ◽  
Kwon Taek Lim
Keyword(s):  
In Vitro Release ◽  
Ester Group ◽  
Water Soluble ◽  
Controlled Delivery ◽  
Hydrophobically Modified ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Vitro Release ◽  
Potential Use

Hydrophobically modified derivative of a γ-cyclodextrin, functionalized with perfluoro alkyl ester group, was prepared and investigated for its potential use as a sustained release carrier for water-soluble drug molsidomine, a peripheral nitrovasodilator used in the treatment of angina pectoris. The molecular encapsulation of molsidomine by the amphiphilic cyclodextrin, octakis(6-O-perfluorobutanoyl)-γ-cyclodextrin (γ-CyD-F), was confirmed by DSC and XRD studies. The in-vitro release of molsidomine from peanut oil suspensions into aqueous phase was found to be significantly retarded by the complexation with γ-CyD-F, mainly due to the hydrophobic properties of the γ-CyD-F.

FORMULATION AND EVALUATION OF OXICONAZOLE B-CYCLODEXTRIN COMPLEX INCORPORATED TOPICAL GEL

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (06) ◽  
pp. 11-17
Author(s):  
S. S Wagle ◽  
◽  
A. P., Gadad ◽  
P. M. Dandagi ◽  
A. S Patil
Keyword(s):  
Solid Dispersion ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Water Soluble ◽  
Gelling Agent ◽  
Topical Gel ◽  
Drug Content ◽  
Percentage Yield ◽  
Vitro Release

Oxiconazole nitrate is antifungal drug having low solubility. An attempt was made to increase the solubility by solid dispersion technique. Twelve solid dispersion formulations were prepared by solvent evaporation and kneading method using β-cyclodextrin and 2-hydroxypropyl β-cyclodextrin as carrier. In vitro release profiles of all solid dispersions were evaluated and were compared with that of pure drug. Optimized formulation (F-3) was then incorporated in gel using Carbopol 940p as gelling agent. The formulated gel was evaluated for various parameters like percentage yield, drug content, pH, viscosity, spreadability, extrudability, drug content, in vitro drug release, in vitro kinetics, antifungal properties, skin irritation and stability studies. The percentage yield obtained was 98.9% and the pH was 6.83. The viscosity was 50,000cp and also showed good spreadability and extrudability. Drug content was found to be 91.6%. The gel formulation showed in vitro release 92.48% whereas marketed formulation showed 76.66% at the end of 8 hrs. The antifungal activity showed greater zone of inhibition than that of marketed formulation and there was no skin irritation on rats. Hence, complex incorporated in gel can be a potential method to improve the solubility of poorly water soluble drugs.

scholarly journals Carvacrol Prodrugs with Antimicrobial Activity Loaded on Clay Nanocomposites

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1793 ◽  
Author(s):  
Piera Eusepi ◽  
Lisa Marinelli ◽  
Fátima García-Villén ◽  
Ana Borrego-Sánchez ◽  
Ivana Cacciatore ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Intestinal Tract ◽  
In Vitro Release ◽  
Water Soluble ◽  
Clay Nanocomposites ◽  
X Ray ◽  
Release Studies ◽  
Wide Range ◽  
Vitro Release

Background: Carvacrol, an essential oil with antimicrobial activity against a wide range of pathogens, and its water soluble carvacrol prodrugs (WSCP1-3) were intercalated into montmorillonite (VHS) interlayers to improve their stability in physiological media and promote their absorption in the intestine. Methods: Intercalation of prodrugs by cation exchange with montmorillonite interlayer counterions was verified by X-ray powder diffraction and confirmed by Fourier transform infrared spectroscopy and thermal analysis. Results: In vitro release studies demonstrated that montmorillonite successfully controlled the release of the adsorbed prodrugs and promoted their bioactivation only in the intestinal tract where carvacrol could develop its maximum antimicrobial activity. The amount of WSCP1, WSCP2, and WSCP3 released from VHS were 38%, 54%, and 45% at acid pH in 120 min, and 65%, 78%, and 44% at pH 6.8 in 240 min, respectively. Conclusions: The resultant hybrids successfully controlled conversion of the prodrugs to carvacrol, avoiding premature degradation of the drug.

Solid Lipid Nanoparticles and Chitosan-coated Solid Lipid Nanoparticles as Promising Tool for Silybin Delivery: Formulation, Characterization, and In vitro Evaluation

2018 ◽  
Vol 16 (2) ◽  
pp. 142-152 ◽  
Author(s):  
Vieri Piazzini ◽  
Lorenzo Cinci ◽  
Mario D'Ambrosio ◽  
Cristina Luceri ◽  
Anna Rita Bilia ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Solid Lipid Nanoparticles ◽  
Cell Monolayer ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Burst Release ◽  
Solid Lipid ◽  
Vitro Release

Background: Silybin (Sb) is the major flavolignan of the extract of Silybum marianum. It is used for the treatment of various acute and chronic liver toxicities, inflammation, fibrosis and oxidative stress. Many studies indicate that Sb is also active against different carcinomas and it has been very recently proposed to be beneficial in type 2 diabetes patients. However, Sb is a low water soluble and low permeable compound. Objective: In this study, Solid Lipid Nanoparticles (SLNs) were proposed to enhance the solubility and the intestinal absorption of Sb. </P><P> Methods: SLNs were made of stearic acid and Brij 78 and subsequently coated with chitosan. Formulations were physically and chemically characterized. Stability studies were also assessed. Sb in vitro release was evaluated in different pH media. In vitro permeability test with artificial membranes and Caco-2 cells were performed. Cellular uptake and mucoadhesion studies were conducted. Results: Both nanoparticles were found to be stable. In vitro release indicated that SLNs may prevent burst release and gastric degradation of Sb. Higher extent of Sb permeation was observed for both nanoparticles in PAMPA and Caco-2 cell monolayer models. The results of the cellular uptake study suggested the involvement of active endocytic processes. Chitosan significantly improves mucoadhesion properties of nanoparticles. </P><P> Conclusions: Together with the excellent stability, strong mucoadhesive property, and slow release, chitosan coated SLNs demonstrated promising potential to enhance absorption of hydrophobic Sb after oral administration.

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