Preparation and Characterization of Monodisperse Mesoporous SiO2 Microspheres Modified by Octaphenylpolyoxyethyiene

2020 ◽  
Vol 987 ◽  
pp. 99-104
Author(s):  
Bo Chen ◽  
Yong Biao Guo ◽  
Yong Peng Huang ◽  
Hui Zhong
Keyword(s):  
Electrostatic Force ◽  
Drug Loading ◽  
Particle Diameter ◽  
Active Surface ◽  
Environmental Water ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Pressure Infiltration ◽  
Specific Pore Volume ◽  
Model Drug

Monodisperse mesoporous SiO2 microsphere is a potential fine candidate carrier of dry powder inhalation, but large numbers of active surface hydrophilic hydroxyls enhance surface energy, hydrogen bonding and electrostatic force, environmental water adsorption and particle agglomeration. Conventional hydrophobic modification of surface hydroxyls, which is conducive to solve the above-mentioned disadvantages, will limit the loading of water-soluble drugs and the drug dissolution in water simultaneously. In this study, monodisperse mesoporous SiO2 microspheres were prepared as carrier and modified innovatively by amphiphilic modifier octaphenylpolyoxyethyiene and 3-aminopropyltriethoxysilane, particle diameter about 60 nm, mean pore size 21.4 nm, specific pore volume 0.95 cm3/g, and specific surface area 130 m2/g. Model drug pentoxyverine citrate was loaded by pressure infiltration and spray drying process, drug loading 8.24%, repose angle 34°, mass median aerodynamic diameter 1.03 μm, and more than 90% of drug could dissolve within 30 min both in water and organic solvents.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

scholarly journals Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

2018 ◽  
Vol 8 (6-s) ◽  
pp. 5-8 ◽  
Author(s):  
Rinshi Agrawal ◽  
RK Maheshwari
Keyword(s):  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Dsc Studies ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Soluble Drug ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

scholarly journals Hyaluronan Self-Agglomerating Nanoparticles For Non- Small Cell Lung Cancer Targeting

2021 ◽  
Author(s):  
Joo-Eun Kim ◽  
Young-Joon Park
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Anticancer Agents ◽  
Drug Loading ◽  
Particle Diameter ◽  
Small Cell ◽  
Water Soluble ◽  
Small Cell Lung ◽  
Water Soluble Drug

Abstract Background: Research into nano-anticancer agents containing water-soluble drug is limited, and no related nano-based anticancer drugs have been developed. In this study, we aimed to develop irinotecan-loaded self-agglomerating hyaluronan nanoparticles (ISHNs) with a high hydrophilic anticancer drug-loading capacity and tumor cell-targeting capability to selectively adhere to overexpressed CD44 on the surface of tumor cells. Results: The ISHNs, comprising hyaluronic acid as a targeting moiety, ferric chloride as a binder, and D-glutamic acid as a stabilizer, self-agglomerated via chelating bonding and were lyophilized using a freeze dryer. The particle diameter and zeta potential of the ISHNs were 93.8 ± 4.48 nm and -36.3 ± 0.28 mV, respectively; a relatively narrow size distribution was observed. The drug fixation yield and drug-loading concentration were 58.3% and 1.75 mg/mL, respectively. Affinity studies revealed a 10-fold stronger targeting to H23 (cluster of differentiation 44 [CD44]+) non-small-cell lung cancer cells than A549 (CD44-) cells.Conclusion: Thus, we developed irinotecan-loaded ISHNs, which comprised irinotecan HCl as a water-soluble anticancer agent, HA as a targeting moiety, FeCl3 as a binder for self-agglomeration, and GA as a stabilizer; HA is a binding material for CD44 on the NSCLC cells. Owing to their ease of manufacture, excellent stability, and CD44-targeting ability, they are a potential nanocarrier for passive and active tumor targeting.

scholarly journals Preparation of silk fibroin microspheres by emulsificationdiffusion method for controlled release drug delivery applications

e-Polymers ◽  
2011 ◽  
Vol 11 (1) ◽  
Author(s):  
Thanonchat Imsombut ◽  
Mangkorn Srisa-ard ◽  
Prasong Srihanam ◽  
Yodthong Baimark
Keyword(s):  
Drug Release ◽  
Silk Fibroin ◽  
Drug Loading ◽  
Water Soluble ◽  
Random Coil ◽  
Diffusion Method ◽  
Surface Erosion ◽  
Erosion Processes ◽  
Release Drug ◽  
Model Drug

AbstractSilk fibroin (SF) microspheres containing a model drug were prepared by a simple water-in-oil emulsification-diffusion method. Aqueous SF solution and ethyl acetate were used as water and oil phases, respectively. Methylene Blue was used as a water-soluble model drug. Effect of drug content on microsphere characteristics, drug loading efficiency and drug release behavior was determined. Scanning electron microscopy revealed that drug-loaded SF microspheres were spherical in shape with a smooth surface. The SF microspheres showed predominant random coil SF conformation. All drug loading efficiencies were approximately 50%. An increase in drug/SF ratio could lead to an increase in %drug release and surface erosion after the drug release test. Drug release from SF microspheres is due to SF matrix swelling and surface erosion processes.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

Self Microemulsifying Nutraceutical and Drug Delivery Systems

2014 ◽  
Vol 7 (3) ◽  
pp. 2520-2528 ◽  
Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
The Novel ◽  
Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

Application of Plakett-Burman Screening Design in Optimization of Process Parameters for Formulation of Canaglifozin Nanosuspension

2020 ◽  
Vol 13 (6) ◽  
pp. 5208-5216
Author(s):  
Nisha Patel ◽  
Hitesh A Patel
Keyword(s):  
Particle Size ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Water Soluble ◽  
Pareto Chart ◽  
Independent Variables ◽  
Mean Particle Size ◽  
Screening Design ◽  
Stirring Time ◽  
Response Variables

In this study, we sought to improve the dissolution characteristics of a poorly water-soluble BCS class IV drug canaglifozin, by preparing nanosuspension using media milling method. A Plackett–Burman screening design was employed to screen the significant formulation and process variables. A total of 12 experiment were generated by design expert trial version 12 for screening 5 independent variables namely the amount of stabilizer in mg (X1), stirring time in hr (X2), amt of Zirconium oxide beads in gm (X3), amount of drug in mg (X4) and stirring speed in rpm (X5) while mean particle size in nm (Y1) and drug release in 10 min. were selected as the response variables. All the regression models yielded a good fit with high determination coefficient and F value. The Pareto chart depicted that all the independent variables except the amount of canaglifozin had a significant effect (p<0.001) on the response variables. The mathematical model for mean particle size generated from the regression analysis was given by mean particle size = +636.48889 -1.28267 amt of stabilizer(X1) -4.20417 stirring time (X2) -7.58333 amt of ZrO2 beads(X3) -0.105556 amt of drug(X4) -0.245167 stirring speed(X5) (R2=0.9484, F ratio=22.07, p<0.001). Prepared canaglifozin nanosuspension exemplified a significant improvement (p<0.05) in the release as compared to pure canaglifozin and marketed tablet with the optimum formulation releasing almost 80% drug within first 10min. Optimized nanosuspension showed spherical shape with surface oriented stabilizer molecules and a mean particle diameter of 120.5 nm. There was no change in crystalline nature after formulation and it was found to be chemically stable with high drug content.

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