scholarly journals FABRICATION AND EVALUATION OF ORAL CONTROLLED RELEASE OF MUCOADHESIVE ALGINATE MICROBEADS CONTAINING FLUVASTATIN SODIUM

2019 ◽  
pp. 101-112
Author(s):  
VENKATA RAMANA REDDY K ◽  
NAGABHUSHANAM MV
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Transport Mechanism ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
Polymer Mixture ◽  
Infrared Spectroscopic Study ◽  
Alginate Concentration ◽  
Curing Agents

Objective: The aim of this study is to prepare oral controlled release (CR) of mucoadhesive alginate microbeads encapsulating fluvastatin by gastroretention technology. Methods: The mucoadhesive microbeads containing fluvastatin were produced using emulsification internal gelation technique. The effect of different variables such as sodium alginate concentration and its combination with other hydrophilic polymers, and the effect of various curing agents on particle size, entrapment efficiency, and in vitro studies were evaluated. Results: There was no marked change in drug entrapment efficiency, and dissolution studies occur during the stability studies of fluvastatin. The in vitro results give data that improvement in the CR of the drug from microbeads compared with marketed tablet. Hence, in this regard, to minimize the frequency of drug administration to reduce side effects. The optimum condition for the preparation of stable alginate beads and produce CR manner was occurred at a higher concentration of combined polymer mixture in equal ratios, i.e., 3% w/v. Infrared spectroscopic study (Fourier transform infrared) confirmed the no incompatibility between drug and other excipients. X-ray diffraction study and differential scanning calorimetry were provided evidence that successful entrapment of drug into the alginates microbeads and drug converted into amorphous nature. The efficiency of mucoadhesion strength of microbeads was determined by wash-off study. Conclusion: The kinetic modeling of the release data indicates drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism. Drug release is a function of pH dependent and controlled drug release depends on type and concentration of polymer blend and curing agents. The release kinetics of drug from the alginate beads followed zero order.

scholarly journals STUDY ON THE EFFECT OF ALGINATE, TYPE OF CROSS LINKERS, AND MUCOADHESIVE POLYMERS ON DRUG RELEASE FROM LOVASTATIN-LOADED MUCOADHESIVE CROSS-LINKED MICROBEADS

2019 ◽  
pp. 246-256
Author(s):  
VENKATA RAMANA REDDY K ◽  
NAGABHUSHANAM MV
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Transport Mechanism ◽  
Alginate Beads ◽  
Hydrophilic Polymers ◽  
Polymer Mixture ◽  
Infrared Spectroscopic Study ◽  
Alginate Concentration ◽  
Sem Studies

Objective: The aim of the current study is to prepare and lovastatin-loaded alginate microbeads were prepared using emulsification gelation internal method by the use of different cross-linking agents, polymer effect in different concentrations on drug release and its combination with hydrophilic polymers on drug release. Methods: The effect of sodium alginate concentration and its combination with other hydrophilic polymers on particle size and shape, scanning electron microscopy (SEM) studies, entrapment efficiency, Fourier transform infrared (FTIR) analysis (FTIR), differential scanning calorimetry (DSC) studies, and X-ray diffraction (XRD) studies conducted to determine compatibility of drug and used excipients and in vitro drug release was studied. The efficiency of mucoadhesion strength of microbeads is determined by wash-off study. Results: The optimum condition for preparation alginate beads and produces sustained release manner was occurred at 3% polymer mixture. Infrared spectroscopic study confirmed the presence of compatibility between drug-polymer additives, good drug entrapment, and SEM studies prove microbeads were in spherical and rough particles. XRD and DSC were used to confirm successful entrapment of drugs into the alginates microbeads. The in vitro release profile could be altered notably by changing formulation parameters to give a sustained release of drug from the microbeads. Conclusion: The kinetic modeling of the release data indicate that drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism and drug release is controlled by both swelling and relaxation of the polymer chains. It was found to be drug release is pH dependent. This will help in overcoming the drawbacks of lovastatin with a short half-life, improves the bioavailability. The release kinetics of drug from the alginate beads followed zero order.

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

2021 ◽  
pp. 5775-5780
Author(s):  
Farhana Sultan ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Production Yield ◽  
In Vitro Drug Release ◽  
Eudragit Rs ◽  
Diffusion Studies

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

scholarly journals EUDRAGIT COATED ALGINATE BEADS BEARING OXALIPLATIN LOADED LIPOSOMES: FORMULATION, OPTIMIZATION AND IN VITRO CHARACTERIZATION

2021 ◽  
pp. 170-177
Author(s):  
ANKITA TIWARI ◽  
SANJAY K. JAIN
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
Molar Ratio ◽  
Specific Drug ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Vesicle Size

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.

scholarly journals Formulation and Evaluation of Controlled Release Maintenance Dose Loaded Niosomes of Anti-Hypertensive Drug

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Chandani Makvana ◽  
Satyajit Sahoo
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Vesicle Size ◽  
Drug Content ◽  
Span 60

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

Development and Evaluation of Olmesartan Medoxomil Controlled Release Floating Microspheres using Natural Gums

2017 ◽  
Vol 10 (4) ◽  
pp. 3788-3794
Author(s):  
Ravi Kumar Kota ◽  
Suresh Gande
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Olmesartan Medoxomil ◽  
In Vitro Dissolution ◽  
Coupled Diffusion ◽  
Intact Surface

The present research was aimed to prepare Olmesartan medoxomil floating microspheres for controlled release using polymers such as sodium alginate, sodium bicarbonate, calcium chloride, Hydroxy propyl methyl cellulose (HPMC K4M, K15M), Olibanum gum and Xanthan gum by ionotropic gelation method. The prepared microspheres were evaluated for the percent drug content, entrapment efficiency, percentage buoyancy and in vitro dissolution studies. Among all the formulations F14 was selected as optimized formulation based on the micromeretic and physico-chemical parameters including drug release studies. Percentage buoyancy of optimized formulation was found to be 96.45%. In vitro release study of formulation F14 showed 98.11% drug release after 12 h in a controlled manner, which is desired for disease like Hypertension.  The reference standard shows the drug release of 94.12% within 12 h. Drug and excipient compatibility studies were carried out by FT-IR and no interactions were observed. The SEM of microspheres show a hollow spherical structure with a rough surface morphology. Some of microspheres showed dented surface structure but they showed good floating ability on medium indicated intact surface. The shell of microspheres also showed some porous structure which might be due to release of carbon dioxide. F14 followed zero order, Higuchi and Korsmeyer Peppas kinetics indicating diffusion controlled with non-fickian (anomalous) transport, projecting that its active ingredient are delivered by coupled diffusion and erosion. From these results, it can be concluded that the polymer proportion controlled the drug release from the olmesartan floating microspheres. 

Formulation and Evaluation of Spray Dried Microspheres of Controlled Release Ramipril

2018 ◽  
Vol 11 (2) ◽  
pp. 4059-4066
Author(s):  
Chetankumar Mutagond ◽  
Vinod M R ◽  
Vijapure V M ◽  
Marapur S C ◽  
R G Patil ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Controlled Released ◽  
Spray Dried

The present study sought to develop and evaluate spray-dried microspheres of chitosan and xanthan gum for controlled release of ramipril, a widely used antihypertensive drug. The prepared microspheres were characterized by particle size analysis, scanning electron microscopic studies, differential scanning calorimetric analysis, Fourier transform infrared spectroscopy analysis, X-ray diffraction studies, drug entrapment efficiency, and in-vitro drug release study. The prepared microspheres were spherical in shape and freely flowing. The size of the microspheres was in the range of 25.7 to 47.4 µm and the drug entrapment efficiency was in the range of 74.68% to 90.44%. TheDSC analysis and X-ray diffraction studies indicated that the drug was uniformly dispersed in amorphous state in the microspheres. The in-vitro drug release indicated that the spray-dried microspheres prepared with chitosan alone were not suitable for controlled released delivery of drug as maximum amount of drug was released within 5 hrs. Whereas microspheres prepared by xanthan gum released small amount of drug within 5 hrs and more amount of drug was controlled released that fit the therapeutic needs. Drug release mechanism followed non-Fickian transport. These suggest the formulation potential of chitosan and xanthan gum for spray-dried microspheres for controlled release of ramipril

scholarly journals Formulation and Evaluation of Eudragit Rl100 Polymeric Drug Loaded Microsponge for Ophthalmic Use

2021 ◽  
pp. 45-51
Author(s):  
Rajashri B. Ambikar ◽  
Ashok V. Bhosale
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Drug Release ◽  
Delivery System ◽  
Diffusion Mechanism ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Drug Content

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles. Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM. Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%.  Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure. Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

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