scholarly journals Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations

2009 ◽  
Vol 59 (3) ◽  
pp. 313-323 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Ch. Patra ◽  
V. Patro ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Research Work ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Physical Parameters ◽  
Drug Solubility ◽  
Significant Difference ◽  
Insoluble Drugs ◽  
Kinetics Of

Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.

scholarly journals EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY

2021 ◽  
pp. 114-121
Author(s):  
S. DUBEY ◽  
S. P. VYAS
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Particle Diameter ◽  
Release Profile ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and characterize paclitaxel (Ptx) loaded sterically stabilized emulsomes to provide non-toxic and biocompatible carriers with high Ptx loading efficiency. Methods: Plain (P-Es) and sterically stabilized emulsomes (SS-Es) were prepared by a modified solvent evaporation method using tristearin as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/ tristearin ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein. Results: The emulsomes so formed were uniform in size with a mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulations showed pH dependent drug release with a slow and sustained release profile. Slower drug release was observed from sterically stabilized emulsomes than the plain emulsomes. The drug release profile followed the Higuchi model with the Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption. Conclusion: The sterically stabilized emulsome can serve as a novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water-soluble drugs as well.

scholarly journals SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (1) ◽  
pp. 79 ◽  
Author(s):  
Surya Teja Sp ◽  
Mothilal M. ◽  
Damodharan N ◽  
Jaison D
Keyword(s):  
Drug Release ◽  
Design Of Experiments ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Substantial Effect ◽  
Fickian Diffusion ◽  
Vesicle Size ◽  
Zero Order Kinetics ◽  
Significant Difference ◽  
Span 60

Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32 full factorial design.Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable.

Mathematical Modeling of Drug Release from Spherical Drug Particles: Analysis of the Effect of Absorption Rate on Drug Release Rate

2009 ◽  
Vol 4 (5) ◽  
Author(s):  
Norman W Loney ◽  
Ramana Susarla
Keyword(s):  
Drug Release ◽  
Absorption Rate ◽  
Release Kinetics ◽  
Closed Form Solution ◽  
Form Solution ◽  
Proposed Model ◽  
Significant Difference ◽  
Rate Of Absorption ◽  
Kinetics Of ◽  
And Diffusion

A closed form solution has been obtained for the release kinetics of a solute from a spherical drug matrix into a finite volume of liquid, taking into account the effect of rate of absorption. The proposed model results clearly show the effect of the absorption rate constant on the rate of drug release. The obtained results are compared with the experimental data and diffusion-only model results. There is a significant difference in the release profile when the rate of absorption of drug is slow. The most important feature of the mathematical relationship between the liquid concentration verses time is its ability to predict change in the performance of the drug by manipulating the parameters of the equation. These parameters include the initial concentration of the drug, the radius of the drug and diffusivity of the drug in the solid to name a few. Therefore, a substantial number of experiments can be eliminated when the optimal performance of a drug is sought after.

scholarly journals OPTIMIZED DELIVERY OF DICLOFENAC SODIUM FORMULATED IN A SUSTAINED RELEASE RAPHIA AFRICANA HYDROCOLLOID MATRIX

2018 ◽  
Vol 10 (1) ◽  
pp. 109
Author(s):  
Musiliu Adedokun ◽  
Clement Nkanta
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Diclofenac Sodium ◽  
Research Work ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Flow Properties ◽  
Weight Variation ◽  
Significant Difference

Objective: The aim of this research work was to comparatively study various proportions of a natural hydrocolloid-Raphia africana, and polyvinylpyrrolidone (PVP) as release sustaining agents in diclofenac sodium tablet formulation.Methods: The purified hydrocolloid (R. africana) was characterized by evaluating its organoleptic, physicochemical and flow properties. Diclofenac-polymer ratios of 1:0, 1:0.2, 1:0.4, 1:0.6, and 1:0.8 were employed to produce different granule batches using wet granulation method (that is, the drug was formulated with 0, 5, 10, 15 and 20 % w/w of either R. africana hydrocolloid or PVP, and coded DWB-00, DRA-05, DRA-10, DRA-15, DRA-20, DPP-05, DPP-10, DPP-15 and DPP-20, respectively). Flow properties of granules were studied by determining bulk density, tapped density, Carr’s index, and Hausner’s ratio for all the formulations. Compressed tablets were evaluated using various parameters as weight variation, friability, hardness, tablet thickness and diameter, content uniformity and in vitro dissolution evaluated in phosphate buffer (pH 7.3).Results: Flowability, mechanical and release parameters determined were within pharmacopoeial limits. Generally, the values of bulk and tapped densities increase as binder concentrations increase for both PVP and R. africana hydrocolloid. The values were significantly different across the batches (p<0.05). Hardness values obtained varied significantly (p<0.05) and were between 5 and 12 KgF which imply that most of the tablet batches are harder than normal depending on the proportion of the polymer used. All the batches exhibited friability within the standard limit without significant difference in values (p>0.05), indicating that tablet formulated with the experimental binders would not undergo surface abrasion. All the formulations exhibited zero order kinetics except batches DPP-10 and DPP-15 which showed Higuchi mechanism. Formulation batches DRA-05 and DRA-10 showed maximum drug release of 98% and 95% respectively after 6 h. A prolonged drug release was observed on increasing polymer ratio. Significantly higher release rates (p<0.05) were observed in the tablets formulated with PVP than those containing R. africana gum. All the batches followed non-fickian diffusion release mechanism.Conclusion: From the study, purified R. africana hydrocolloid generally appeared to perform better than PVP as sustained release agent.

scholarly journals Formulation and Evaluation of Release Kinetics of Diltiazem Hydrochloride from Kollicoat SR 30 D Coated Pellets Prepared by Air Suspension Technique

1970 ◽  
Vol 43 (3) ◽  
pp. 321-332
Author(s):  
Afsana Akhter ◽  
Monzurul Amin Roni ◽  
Mohammad Shahriarul Absar ◽  
Golam Kibria ◽  
Reza-ul Jalil
Keyword(s):  
Polyvinyl Acetate ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Physical Parameters ◽  
Diltiazem Hydrochloride ◽  
Significant Difference ◽  
Kinetics Of

The purpose of the present study is to investigate the effect of polyvinyl acetate on the release kinetics of diltiazem hydrochloride from coated pellets prepared by solution and suspension layering technique. Kollicoat SR 30 D, an aqueous dispersion of polyvinyl acetate with different weight ratios was chosen to sustain the release of the drug. Drug was loaded with hydroxypropyl methyl cellulose on nonpareil seeds then coated with the Kollicoat SR 30 D. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. No significant difference was found in drug release from uncoated pellets and the pellets coated with 5% polymer load. With 10% polymer load, the initial release was minimized but from 2nd hour the release was quick-tempered. Better sustaining effect was found from 15- 20% polymer loaded pellets. The mean dissolution time was 2.5h and 4h while the polymer load was 15% and 20% respectively. Also these two cases 80% drug was released at 6h and 9h respectively. The physical parameters of the prepared pellets were also compared in this study. The release of drug from the coated pellets appeared to follow Higuchi's release kinetics.Key words: Diltiazem, Pellets, Kollicoat SR 30 D, Aqueous coating, Physical parameters, Release kinetics.DOI = 10.3329/bjsir.v43i3.1147Bangladesh J. Sci. Ind. Res. 43(3), 321-332, 2008

scholarly journals FORMULATION AND IN VITRO EVALUATION OF RAMELTEON TABLETS FOR COLON DRUG DELIVERY SYSTEM BY COMPRESSION COATING

2021 ◽  
pp. 249-253
Author(s):  
TRINADHA RAO M. ◽  
PARIMALA Y. ◽  
YAMINI M. ◽  
PHANINDRA CVS ◽  
SRINIVASA RAO Y.
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Flow Property ◽  
Fickian Diffusion ◽  
In Vitro Drug Release ◽  
First Order Kinetics ◽  
Colon Drug Delivery ◽  
Compression Coating ◽  
Kinetics Of

Objective: Ramelteon, is a sleep agent that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABAA receptors. In the present research work, the formulation of ramelteon targeted to colon by using various polymers developed. Methods: Colon-targeted tablets were prepared in two steps. Initially, core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethylcellulose, Eudragit RLPO and L100 were used as enteric coating polymers. The precompression blend of all formulations was subjected to various flow property tests and all the formulations were passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to physical characterization, drug content, in vitro drug release and kinetics of drug release. Results: Among all the formulations, F4 formulation was found to be optimized as it was retarded the drug release up to 18 h and showed maximum of 99.25% drug release. It followed the first-order kinetics mechanism. All the formulations having Korsmeyer-Peppas ‘n’ values are in the range of 0.540 to 0.818. Hence, it was concluded that the prepared formulations followed non-Fickian diffusion. Conclusion: An effective and stable remelteon colon targeted formulation developed for treating insomnia.

Formulation and Evaluation of Lovastatin Loaded Nanosponges for the treatment of Hyperlipidemia

2021 ◽  
pp. 5653-5660
Author(s):  
Ranjitha R ◽  
Elango K ◽  
Devi Damayanthi R ◽  
Sahul Hameed Niyaz U
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Flow Property ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Average Particle ◽  
Stability Studies ◽  
Formulation Parameters

The present investigations was aimed to improve the solubility, to release the drug in a controlled manner for extended period of time, reduce dose dependent side effects and improve the bioavailability of a poorly water soluble BCS class II drug of Lovastatin by formulating it as Nanosponges drug delivery system. Lovastatin Nanosponges were formulated by emulsion solvent evaporation method using Eudragit RS 100 and Ethyl Cellulose as a polymers, PVA as a stabilizer and finally enclosed in hard gelatin Capsules. The prepared Nanosponges were evaluated for FTIR, particle size, polydispersity index (PDI), zeta potential, morphological characteristics by scanning electron microscopy (SEM), production yield, entrapment efficiency, solubility studies, in vitro drug release studies, release kinetics study, stability studies, Flow property and porosity. The optimized formulation filled in capsules and Post formulation parameters of capsule were determined. FTIR studies showed no interaction between drug and excipients. Percentage yield of all the formulation (F1-F10) was found to be in the range of 85.83 to 99.85%. The entrapment efficiency of all the formulations was found to be in the range of 61.68 to 91.18%, among all the formulations F3 (90.04%) and F8 (91.18%) shows high entrapment efficiency. The solubility of all formulation improved (from insoluble to slightly soluble) compared to pure drug of Lovastatin. Among all the formulations F3 (98.15%) and F8 (97.57%) shown complete drug release at the end of 12th hrs. The average particle size of optimized formulation F3 and F8 was found to be 727.0 nm and 769.5 nm respectively. SEM images of optimized formulation showed that the Nanosponges were spherical with numerous pores on their surface, uniform and spongy in nature. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with Non Fickian diffusion. Stability studies indicated that the formulation is stable as per ICH guidelines. The flow property measurements for optimized formulation observed good were its filled in capsules. Post formulation parameters of capsule were comply with official specifications. They concluded that the both polymers used were efficient carriers for Lovastatin Nanosponges.

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.

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

2020 ◽  
Vol 16 ◽  
Author(s):  
Anjali P.B ◽  
Jawahar N. ◽  
Jubie S. ◽  
Neetu Yadav ◽  
Selvaraj A. ◽  
...  
Keyword(s):  
Drug Release ◽  
Phospholipase A2 ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Structural Analog ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
Nanostructured Lipid Carrier ◽  
Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

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