Synthesis of amine functionalized graphite nanosheets and their water-soluble derivative for drug loading and controlled release

2015 ◽  
Vol 39 (4) ◽  
pp. 2451-2458 ◽  
Author(s):  
Amrita Chakravarty ◽  
Koushik Bhowmik ◽  
Goutam De ◽  
Arnab Mukherjee
Keyword(s):  
Controlled Release ◽  
Drug Loading ◽  
Water Soluble ◽  
Chemical Functionalization ◽  
Graphite Nanosheets ◽  
Amine Functionalized

Amine functionalized graphite nanosheets are formed by facile chemical functionalization and their water soluble PEGylated derivative is prepared for drug loading and controlled release.

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GELUCIRE BEADS OF ANTIHYPERTENSIVE DRUG FOR FLOATING DRUG DELIVERY SYSTEM USING 32 FACTORIAL DESIGNS

2021 ◽  
pp. 150-156
Author(s):  
KHUSHBOO RANKA ◽  
KAMAL S RATHORE
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Loading ◽  
Linear Regression Analysis ◽  
Extended Period ◽  
Multiple Linear Regression Analysis ◽  
Water Soluble ◽  
Tween 20 ◽  
Formulation Development ◽  
Floating Drug Delivery

Objective: The aim of this study was to design and to optimize lipid based beads for multiunit floating drug delivery of ramipril. Methods: The beads prepared by melt-solidification method. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of Gelucire (X1) and Tween 20 (X2) as independent variable and the percentage drug release in 1 (Y1), 6 (Y2), and 12 h (Y3) as dependent variable. Gelucire 43/01 has chosen for release retardant and Tween 20 for solubility enhancement and drug loading agent. Results: The results of multiple linear regression analysis indicated that for obtain a floating drug delivery, the optimum concentrations of both the lipid and drug loading agent should be used. The factorial models were used to prepare optimized floating beads and optimized formulations showed controlled release profiles for the extended period of more than 12 h. Conclusion: From the study, it was concluded that beads of Gelucire for sparingly water-soluble drug ramipril can provide controlled release for extended period.

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

Microsponges: An Overview

2017 ◽  
Vol 4 (4) ◽  
Author(s):  
Hamid Hussain ◽  
Divya Juyal ◽  
Archana Dhyani
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Active Agent ◽  
Topical Delivery ◽  
Water Soluble ◽  
Wide Range ◽  
Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

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.

Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

2020 ◽  
Vol 16 ◽  
Author(s):  
Poovi Ganesan ◽  
N Damodharan
Keyword(s):  
Orthogonal Array ◽  
Drug Loading ◽  
Optimization Technique ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Orthogonal Array Design ◽  
Formulation Development ◽  
Array Design ◽  
Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

scholarly journals The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 455
Author(s):  
Emilia Szymańska ◽  
Katarzyna Woś-Latosi ◽  
Julia Jacyna ◽  
Magdalena Dąbrowska ◽  
Joanna Potaś ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Drug Loading ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Complex Nature ◽  
Prolonged Release ◽  
Scanning Calorimetry ◽  
Burst Effect ◽  
The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

A novel anhydrous preparation of PEG hydrogels enables high drug loading with biologics for controlled release applications

2021 ◽  
Vol 147 ◽  
pp. 110286
Author(s):  
Christian E. Ziegler ◽  
Moritz Graf ◽  
Sebastian Beck ◽  
Achim M. Goepferich
Keyword(s):  
Controlled Release ◽  
Drug Loading ◽  
Peg Hydrogels ◽  
High Drug ◽  
High Drug Loading

scholarly journals Novel Drug Delivery Device Using Silicone: Controlled Release of Insoluble Drugs or Two Kinds of Water-Soluble Drugs

2003 ◽  
Vol 51 (1) ◽  
pp. 15-19 ◽  
Author(s):  
Masako Kajihara ◽  
Toshihiko Sugie ◽  
Hiroo Maeda ◽  
Akihiko Sano ◽  
Keiji Fujioka ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Water Soluble ◽  
Delivery Device ◽  
Drug Delivery Device ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Novel Drug
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