scholarly journals Development of Theophylline Microbeads Using PregelatinizedBreadfruit Starch (Artocarpus altilis) as a Novel Co-polymer for Controlled Release

2019 ◽  
Vol 9 (1) ◽  
pp. 93-101 ◽  
Author(s):  
Adenike Okunlola ◽  
Shukuralilahi Abidemi Adewusi
Keyword(s):  
Size Range ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Controlled Delivery ◽  
Dissolution Time ◽  
Thermal Flow ◽  
Artocarpus Altilis ◽  
Microsphere Size ◽  
Time Required ◽  
Orderly Arrangement

Purpose: The aim of this study was to prepare formulations of theophylline microbeads usingpregelatinized breadfruit starch (Artocarpus altilis, family Moraceae) in combination withsodium alginate and chitosan at various polymer: drug ratios. Microbead formulations forcontrolled delivery of theophylline would be better alternatives to conventional dosage formsfor optimized drug therapy.Methods: The native and pregelatinized starches were characterized for morphology (scanningelectron microscope), crystallinity (Fourier transform intra-red spectroscopy, FTIR and X-raydiffractometer, XRD), thermal flow (differential scanning colorimeter), density and flowproperties. Theophylline microbeads were prepared by ionic gelation and characterized usingsize, swelling index, entrapment efficiency and time required for 15% and 50% drug release (t15and t50 respectively).Results: FTIR and XRD spectra revealed the orderly arrangement of granules of the semi-crystallinebreadfruit starch was disrupted on gelatinization. The viscosity and flow of pregelatinized starchwere enhanced. Theophylline microbeads were near spherical in shape with size range 1.09± 0.672 to 1.58 ± 0.54 mm. FTIR and XRD spectra confirmed there was no drug-polymerinteraction. Microsphere size, swelling increased while entrapment and dissolution time (t50)reduced with polymer: drug ratio. The entrapment efficiency ranged from 30.99 ± 1.32 to 78.50± 2.37%. Optimized formulation, starch: alginate ratio 3:1 at polymer: drug ratio of 2:1, gave aprolonged dissolution time (t50 = 8.40 ± 1.20 h).Conclusion: Breadfruit starch was suitable as a copolymer for the controlled delivery oftheophylline in microbeads which could serve as a substitute to synthetic polymers in drugdelivery.

scholarly journals Entrapment of the Fastest Known Carbonic Anhydrase with Biomimetic Silica and Its Application for CO2 Sequestration

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2452
Author(s):  
Chia-Jung Hsieh ◽  
Ju-Chuan Cheng ◽  
Chia-Jung Hu ◽  
Chi-Yang Yu
Keyword(s):  
Carbonic Anhydrase ◽  
High Activity ◽  
Co2 Sequestration ◽  
Residual Activity ◽  
Entrapment Efficiency ◽  
Free Form ◽  
Uncatalyzed Reaction ◽  
The Stability ◽  
Time Required

Capturing and storing CO2 is of prime importance. The rate of CO2 sequestration is often limited by the hydration of CO2, which can be greatly accelerated by using carbonic anhydrase (CA, EC 4.2.1.1) as a catalyst. In order to improve the stability and reusability of CA, a silica-condensing peptide (R5) was fused with the fastest known CA from Sulfurihydrogenibium azorense (SazCA) to form R5-SazCA; the fusion protein successfully performed in vitro silicification. The entrapment efficiency reached 100% and the silicified form (R5-SazCA-SP) showed a high activity recovery of 91%. The residual activity of R5-SazCA-SP was two-fold higher than that of the free form when stored at 25 °C for 35 days; R5-SazCA-SP still retained 86% of its activity after 10 cycles of reuse. Comparing with an uncatalyzed reaction, the time required for the onset of CaCO3 formation was shortened by 43% and 33% with the addition of R5-SazCA and R5-SazCA-SP, respectively. R5-SazCA-SP shows great potential as a robust and efficient biocatalyst for CO2 sequestration because of its high activity, high stability, and reusability.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

2021 ◽  
pp. 5202-5206
Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Drug Bioavailability ◽  
Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

scholarly journals Americium/Curium Extraction from a Lanthanide Borosilicate Glass

1996 ◽  
Vol 465 ◽  
Author(s):  
T. S. Rudisill ◽  
J. M. Pareizs ◽  
W. G. Ramsey
Keyword(s):  
National Laboratory ◽  
Fission Products ◽  
Glass Particle ◽  
Radioactive Isotopes ◽  
Dissolution Time ◽  
Savannah River ◽  
Oak Ridge ◽  
Glass Dissolution ◽  
Time Required ◽  
River Site

ABSTRACTA solution containing kilogram quantities of highly radioactive isotopes of amerícium and curium (Am/Cm) and lanthanide fission products is currently stored in a process tank at the Department of Energy's Savannah River Site (SRS). This tank and its vital support systems are old, subject to deterioration, and prone to possible leakage. For this reason, a program has been initiated to stabilize this material as a lanthanide borosilicate (LBS) glass.1 The Am/Cm has commercial value and is desired for use by the heavy isotope programs at the Oak Ridge National Laboratory (ORNL).A recovery flowsheet was demonstrated using a curium-containing glass to extract the Am/Cm from the glass matrix. The procedure involved grinding the glass to less than 200 mesh and dissolving in concentrated nitric acid at 110°C. Under these conditions, the dissolution was essentially 100% after 2 hours except for the insoluble silicon. Using a nonradioactive surrogate, the expected glass dissolution rate during Am/Cm recovery was bracketed by using both static and agitated conditions. The measured rates, 0.0082 and 0.040 g/hrcm2, were used to develop a predictive model for the time required to dissolve a spherical glass particle in terms of the glass density, particle size, and measured rate. The calculated dissolution time was in agreement with the experimental observation that the curium glass dissolution was complete in less than 2 hr.

scholarly journals Development of coated beads for oral controlled delivery of cefaclor: In vitro evaluation

2013 ◽  
Vol 63 (1) ◽  
pp. 31-44 ◽  
Author(s):  
Bazigha K. Abdul ◽  
Sahar A. Fahmy
Keyword(s):  
Antimicrobial Activity ◽  
Controlled Release ◽  
Dosage Form ◽  
Size Range ◽  
Alginate Beads ◽  
Controlled Delivery ◽  
Peg 400 ◽  
Maximum Value ◽  
Plasma Profile

The aim of the present study was to develop and characterize coated chitosan-alginate beads containing cefaclor as a controlled release delivery system. Coated cefaclor beads were prepared by solvent evaporation techniques. Beads were found to be intact and spherical in shape. Their size range was 1.05 to 2.06. The loading efficiency showed maximum value when the concentration of cefaclor, chitosan and PEG 400 was 10 % (m/V), 0.5 % (m/V) and 2 % (V/V), respectively. Best retardation of cefaclor release from chitosan-alginate beads was achieved by coating with 15 % of shellac in formula F19. A significant antimicrobial activity (p < 0.05) against Staphylococcus aureus and Klebsiella pneumoniae was observed for formula F19 compared to the standard antibiotic disc. Furthermore, the simulated plasma profile showed the superiority of F19 in sustaining drug release for more than 12 h. Therefore, shellac coated chitosan-alginate beads could be considered a successful controlled release oral cefaclor dosage form.

scholarly journals ENHANCEMENT OF THERAPEUTIC WINDOW OF METFORMIN HYDROCHLORIDE BY FABRICATION OF MICROSPHERES COMPRISING POLYMERIC INCULCATION WITH SEMI-SYNTHETIC AND SYNTHETIC POLYMERS BY IMPLEMENTATION OF BOX-BEHNKEN DESIGN

2021 ◽  
pp. 257-264
Author(s):  
MD AAMER QUAZI ◽  
NAZIA KHANAM
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Therapeutic Window ◽  
Metformin Hydrochloride ◽  
Box Behnken Design ◽  
Mean Particle Size

Objective: Innovative enhancement of therapeutic window of Metformin hydrochloride (MFH) and bioavailability through mucoadhesive microspheres by polymeric inculcation of hydroxypropyl methylcellulose K4M grade (HPMC K4M), hydroxypropyl methylcellulose K100M grade (HPMC K100M) and Kollidon SR grade (KS). Methods: Controlled release system was developed by incorporating semi-synthetic and synthetic polymers by modified solvent evaporation technique. Fabrication of mucoadhesive microspheres was designed by the implementation of experimental designs to obtain most optimum concentration of selected factors. The method was optimized by Box Behnken design (BBD) with selected factors as concentrations of semi-synthetic and synthetic polymer with stirring speed influence for the obtained responses that were mean particle size (Y1) entrapment efficiency of drug (Y2) and percent mucoadhesion (Y3). Microspheres were characterized for particle size, entrapment efficiency of drug, ex-vivo mucoadhesion study, in vitro study, Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD) detection and H1 Nuclear magnetic resonance (NMR) quantification for optimized formulation. Results: Implementation of response surface method software for BBD yielded stable microspheres with mean particle size 274 µm, entrapment efficiency of drug 85.07% and percent mucoadhesion 67.03% for optimized formulation F5. Conclusion: Bridging of MFH with the highly innovative combination of semi-synthetic and synthetic polymers yielded stable, cost-effective microspheres with improved bioavailability with controlled-release effect as till date no literature is available that provide information with selected polymeric combination and analytical characterization.

scholarly journals Preparasi dan Karakterisasi Mikroenkapsulasi Asam Mefenamat Menggunakan Polimer Kitosan dan Natrium Alginat dengan Metode Gelasi Ionik

2020 ◽  
Author(s):  
Sandra Aulia Mardikasari
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Active Substance ◽  
Mefenamic Acid ◽  
Size Range ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Gastrointestinal Disorders ◽  
Ionic Gelation ◽  
Inflammatory Drugs

Mefenamic acid belongs to a class of the Non-steroidal Anti-Inflammatory drugs that work as an analgesic. But mefenamic acid can cause gastrointestinal disorders, has unpleasant odors and tastes and sensitive to the influence of light and temperature. Microencapsulation technology is a technique where the active substance is coated by a thin layer so that the active substance is protected from environmental influences. The aim of this research was to formulate and characterize mefenamic acid in the form of microencapsulation using ionic gelation methods. Preparation was done by comparing 3 variations of concentrations of sodium alginate polymers. Success parameters include the entrapment efficiency, particle shape, particle size distribution, and dissolution test. The results showed that the entrapment efficiency  respectively 98,69%,  96,38%  and 93,98%, with spherical shape, and particle size that fulfilled the microencapsulation size range of 1,268 μm, 1,343 μm and 1.386 μm and the release of the active ingredients in an acidic medium of pH 1.2 was 8.811 mg/L, 6.751 mg/L and 5.965 mg/L, also on a base medium of pH 7.4  was 79.908 mg/L, 63.394 mg/L and 40,312 mg/L. So that microencapsulation of mefenamic acid can be prepared with polymer chitosan and sodium alginate using the ionic gelation method.

scholarly journals FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE

2019 ◽  
pp. 438-446
Author(s):  
GOWTHAMI B ◽  
NIHITHA S ◽  
SANTHI PRIYA NAGAM ◽  
RAMA RAO NADENDLA
Keyword(s):  
Fluidized Bed ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Lag Phase ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Coating Technique ◽  
Fluidized Bed Coating

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers. Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer). Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics. Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design.

Pharmacosomes: An approach to improve biopharmaceutical properties of drugs basic considerations in development

2021 ◽  
pp. 4485-4490
Author(s):  
Popat Kumbhar ◽  
Tejaswini Shinde ◽  
Tejaswini Jadhav ◽  
Tejas Gavade ◽  
Rushikesh Sorate ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Stability ◽  
Entrapment Efficiency ◽  
Delivery Systems ◽  
Controlled Delivery ◽  
State Measurement ◽  
High Entrapment Efficiency ◽  
Biopharmaceutical Properties

Vesicular drug delivery systems including niososmes, liposomes, pharmacosomes, transferosomes, electrosomes, ethosomes, etc have been widely accepted for controlled delivery of the drug. Amongst, all these drug delivery systems pharmacosomes are gaining more attention of the researchers due to several benefits such as high entrapment efficiency, improved biopharmaceutical properties, and pharmacokinetic performance, no leakage or loss of drug, stability, etc. Pharmacosomes are amphiphilic phospholipid complexes of drugs having active hydrogen that bind to phospholipids and self-assembled into vesicles in an aqueous medium. Both hydrophilic and lipophilic drugs have been formulated into pharmacosomes that caused improved solubility and permeability of drugs. Pharmacosomes are prepared by using various techniques such as hand shaking method, ether injection, solvent evaporation method, supercritical fluid approach, etc and are characterized for prodrug confirmation, surface morphology, crystal state measurement, in vitro drug release, and stability, etc. Despite wide research and highly encouraging results in the preclinical studies, translation of these nanomedicines from laboratory to market has been very limited. The main aim of this review is to describe comprehensively the potential of pharmacosomes as a vesicular drug delivery system focusing mainly on their conventional and advanced methods of preparation, different characterization techniques, and their applications in the delivery of different types of drugs with improved biopharmaceutical properties and pharmacokinetic performance.

scholarly journals Preparation and Characterization of Polyvinyl Acetate (Kollidon® SR) Microspheres Containing Diclofenac Sodium II: Effect of core loading

1970 ◽  
Vol 8 (2) ◽  
pp. 117-122
Author(s):  
Md Saiful Islam ◽  
Ashfacur Rahman ◽  
Mohammad Kaisarul Ismal ◽  
Jakir Ahmed Chowdhury ◽  
Reza-ul Jalil
Keyword(s):  
Encapsulation Efficiency ◽  
Polyvinyl Acetate ◽  
Drug Loading ◽  
Diclofenac Sodium ◽  
Solvent Evaporation ◽  
Dissolution Time ◽  
Release Rates ◽  
Mean Dissolution Time ◽  
Evaporation Technique ◽  
Microsphere Size

Diclofenac Sodium (DS) loaded Kollidon® SR (Polyvinyl acetate and povidone based matrix retarding polymer) microspheres of different drug loading were prepared using W/O emulsification solvent evaporation technique. Polymeric solution containing the DS was emulsified in light liquid paraffin (LLP) which was initially emulsified by 1% (w/w of the continuum) lipophilic surfactant Span 60. The study was conducted to investigate the effect of different core to polymer ratio (0.5: 1, 1 : 1, 1.5 : 1 and 2 : 1) on microsphere size, encapsulation efficiency and release kinetics of DS. Microsphere size was decreased with increased core loading. However, higher encapsulation efficiency was observed with higher core loading. A square root of time dependent release of DS was observed from the KSR microspheres. Increased core loading caused faster release of DS. Release rates of DS were affected by different DS content in the core. Normalized release rates were also found to be increased with high core loading. Mean dissolution time (MDT) and t50 values were also calculated and were found to be affected significantly by different DS loading to KSR microspheres. Low DS loading increased MDT. Key words: Kollidon® SR; Diclofenac Sodium; Microsphere; Solvent evaporation technique; Mean dissolution time. DOI: 10.3329/dujps.v8i2.6025 Dhaka Univ. J. Pharm. Sci. 8(2): 117-122, 2009 (December)

scholarly journals Partial Surface Modification of Low Generation Polyamidoamine Dendrimers: Gaining Insight into their Potential for Improved Carboplatin Delivery

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 214 ◽  
Author(s):  
Nguyen ◽  
Bach ◽  
Nguyen Tran ◽  
Cao ◽  
Nguyen ◽  
...  
Keyword(s):  
Renal Clearance ◽  
Size Range ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Efficient Delivery ◽  
Methoxypolyethylene Glycol ◽  
Potential Applications ◽  
High Entrapment Efficiency ◽  
Surface Modified

Carboplatin (CAR) is a second generation platinum-based compound emerging as one of the most widely used anticancer drugs to treat a variety of tumors. In an attempt to address its dose-limiting toxicity and fast renal clearance, several delivery systems (DDSs) have been developed for CAR. However, unsuitable size range and low loading capacity may limit their potential applications. In this study, PAMAM G3.0 dendrimer was prepared and partially surface modified with methoxypolyethylene glycol (mPEG) for the delivery of CAR. The CAR/PAMAM G3.0@mPEG was successfully obtained with a desirable size range and high entrapment efficiency, improving the limitations of previous CAR-loaded DDSs. Cytocompatibility of PAMAM G3.0@mPEG was also examined, indicating that the system could be safely used. Notably, an in vitro release test and cell viability assays against HeLa, A549, and MCF7 cell lines indicated that CAR/PAMAM G3.0@mPEG could provide a sustained release of CAR while fully retaining its bioactivity to suppress the proliferation of cancer cells. These obtained results provide insights into the potential of PAMAM G3.0@mPEG dendrimer as an efficient delivery system for the delivery of a drug that has strong side effects and fast renal clearance like CAR, which could be a promising approach for cancer treatment.

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