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.

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 Poly (2-hydroxyethylmethacrylate –co–methylmethacrylate)/Lignocaine Contact Lens Preparation, Characterization, and in vitro Release Dynamic

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 917 ◽  
Author(s):  
Taieb Aouak ◽  
Wassem Sharaf Saeed ◽  
Nawaf M. Al-Hafi ◽  
Abdel-Basit Al-Odayni ◽  
Abdulaziz Ali Alghamdi ◽  
...  
Keyword(s):  
Contact Lens ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Potential Candidate ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Drug Carrier System ◽  
Vitro Release ◽  
Carrier Systems

2-hydroxyethyl methacrylate, methylmethacrylate, ethylene glycol dimethyl methacrylate, and lignocaine (drug) were mixed together and the monomers were copolymerized at 60 °C through a free radical polymerization in the presence of α,α′-Azoisobutyronitrile in tetrahydrofuran. A series of copolymer/drug composites with different monoacrylate monomer compositions were prepared by solvent evaporation and characterized by different methods such as nuclear magnetic resonance, differential scanning calorimetry, Fourier transform infrared, X-ray diffraction, and mechanical and optical testing. The water content in the copolymers and the cell viability test on the samples were also examined in this investigation. The results of the analyses of the properties of this drug-carrier system are promising, indicating that this material may be a potential candidate for contact lens applications. The release dynamic of this medication from the prepared drug-carrier systems was investigated in neutral pH media. The results obtained revealed that the diffusion of lignocaine through the copolymer matrix obeys the Fick model and the dynamic release can be easily controlled by the methyl methacrylate content in the copolymer.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals pH-Responsive Liposomes of Dioleoyl Phosphatidylethanolamine and Cholesteryl Hemisuccinate for the Enhanced Anticancer Efficacy of Cisplatin

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 129
Author(s):  
Hassan Shah ◽  
Asadullah Madni ◽  
Muhammad Muzamil Khan ◽  
Fiaz-ud-Din Ahmad ◽  
Nasrullah Jan ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Release Rate ◽  
In Vitro Release ◽  
Chemotherapeutic Agents ◽  
Ph Responsive ◽  
Scanning Calorimetry ◽  
Cholesteryl Hemisuccinate ◽  
Vitro Release

The current study aimed to develop pH-responsive cisplatin-loaded liposomes (CDDP@PLs) via the thin film hydration method. Formulations with varied ratios of dioleoyl phosphatidylethanolamine (DOPE) to cholesteryl hemisuccinate (CHEMS) were investigated to obtain the optimal particle size, zeta potential, entrapment efficiency, in vitro release profile, and stability. The particle size of the CDDP@PLs was in the range of 153.2 ± 3.08–206.4 ± 2.26 nm, zeta potential was −17.8 ± 1.26 to −24.6 ± 1.72, and PDI displayed an acceptable size distribution. Transmission electron microscopy revealed a spherical shape with ~200 nm size. Fourier transform infrared spectroscopic analysis showed the physicochemical stability of CDDP@PLs, and differential scanning calorimetry analysis showed the loss of the crystalline nature of cisplatin in liposomes. In vitro release study of CDDP@PLs at pH 7.4 depicted the lower release rate of cisplatin (less than 40%), and at a pH of 6.5, an almost 65% release rate was achieved compared to the release rate at pH 5.5 (more than 80%) showing the tumor-specific drug release. The cytotoxicity study showed the improved cytotoxicity of CDDP@PLs compared to cisplatin solution in MDA-MB-231 and SK-OV-3 cell lines, and fluorescence microscopy also showed enhanced cellular internalization. The acute toxicity study showed the safety and biocompatibility of the developed carrier system for the potential delivery of chemotherapeutic agents. These studies suggest that CDDP@PLs could be utilized as an efficient delivery system for the enhancement of therapeutic efficacy and to minimize the side effects of chemotherapy by releasing cisplatin at the tumor site.

scholarly journals Cellulose/guar gum hydrogel microspheres as a magnetic anticancer drug carrier

BioResources ◽  
2019 ◽  
Vol 14 (2) ◽  
pp. 3615-3629 ◽  
Author(s):  
Yanli Li ◽  
Yucheng Feng ◽  
Jun Jing ◽  
Fei Yang
Keyword(s):  
Anticancer Drug ◽  
Guar Gum ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Adsorption Effect ◽  
Magnetic Hydrogel ◽  
Vitro Release ◽  
Hydrogel Microspheres

A novel magnetic anticancer drug carrier based on cellulose, guar gum, and Fe3O4 hydrogel microspheres was synthesized by chemical crosslinking. These microspheres were crosslinked with epoxy chloropropane and loaded with 5-fluorouracil (5-fu). The effect of the ratio of cellulose to guar gum on bead size, drug loading, and in vitro release behaviors were investigated. The influence of the magnetic content on drug loading and in vitro release behaviors were also evaluated. The magnetic hydrogel microspheres were characterized via an optical microscope, Fourier transform infrared spectroscopy, swelling behavior analysis, vibrating sample magnetometer, and ultraviolet absorption spectroscopy. The results showed that as the ratio of cellulose to guar gum increased from 3:1 to 5:1, the particle size increased from 395 to 459 um. Moreover, the drug loading capacity, encapsulation efficiency, and in vitro release behavior were influenced by the ratio of cellulose/guar gum and Fe3O4 content. Finally, the Fe3O4 particle had an adsorption effect on the drug, thereby reducing the maximum cumulative release.

Calcium phosphate porous pellets as drug delivery systems: Effect of drug carrier composition on drug loading and in vitro release

2012 ◽  
Vol 32 (11) ◽  
pp. 2679-2690 ◽  
Author(s):  
Hiva Baradari ◽  
Chantal Damia ◽  
Maggy Dutreih-Colas ◽  
Etienne Laborde ◽  
Nathalie Pécout ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Calcium Phosphate ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Vitro Release

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

Sign in / Sign up

Export Citation Format

Share Document