Synthesis of hybrid polymer blend nanoparticles and incorporation into in situ gel foam spray for controlled release therapy using a versatile synthetic purine nucleoside analogue antiviral drug

RSC Advances ◽  
2015 ◽  
Vol 5 (17) ◽  
pp. 12956-12973 ◽  
Author(s):  
Durai Ramyadevi ◽  
Kalpoondi Sekar Rajan
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Nucleoside Analogue ◽  
Antiviral Drug ◽  
Release Mechanism ◽  
Hybrid Polymer ◽  
In Situ Gel ◽  
Drug Release Mechanism ◽  
Physical Interactions

Antiviral drug loaded nanoparticles is incorporated intoin situgel for controlled release therapy. Chemical and physical interactions of drug and polymers in the system influenced their characteristics and drug release mechanism.

scholarly journals 5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

2020 ◽  
Vol 57 (3) ◽  
pp. 180-188
Author(s):  
Roxana Iancu ◽  
Stefan Andrei Irimiciuc ◽  
Maricel Agop ◽  
Mihail Frasila ◽  
Maria-Alexandra Paun ◽  
...  
Keyword(s):  
Drug Release ◽  
Polarized Light ◽  
Crosslinking Density ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Morphological Aspects ◽  
Drug Release Mechanism ◽  
The Matrix

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

Study of the drug release mechanism from tyrphostin AG-1295-loaded nanospheres by in situ and external sink methods

2002 ◽  
Vol 83 (3) ◽  
pp. 401-414 ◽  
Author(s):  
Michael Chorny ◽  
Ilia Fishbein ◽  
Haim D Danenberg ◽  
Gershon Golomb
Keyword(s):  
Drug Release ◽  
Release Mechanism ◽  
Drug Release Mechanism

scholarly journals Design and Optimization of Thermo-reversible Nasal in situ Gel of Atomoxetine Hydrochloride Using Taguchi Orthogonal Array Design

2019 ◽  
Vol 18 (2) ◽  
pp. 183-193 ◽  
Author(s):  
PK Lakshmi ◽  
K Harini
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Poloxamer 407 ◽  
Release Mechanism ◽  
Gelation Temperature ◽  
In Situ Gel ◽  
Design And Optimization ◽  
Mucoadhesive Polymers ◽  
Carbopol 934P

The present investigation was aimed to develop a thermo-reversible nasal in situ gel of atomoxetine hydrochloride (AH) with reduced nasal muco-ciliary clearance in order to improve residence time and targeting the brain through nasal mucosa for the treatment of attention-deficit hyperactivity disorder (ADHD). In situ gel formulations were prepared using different concentrations of the thermo-gelling poloxamer 407 and mucoadhesive polymers. Temperature-triggered ionic gelation is the mechanism involved. Taguchi L9 OA experimental design was employed for the optimization of the effect of independent variables (Poloxamer 407 and Carbopol 934P) on the response (gelation temperature). In situ gel formulation F4 having 20% poloxamer 407 and 0.3% carbopol 934P and formulation F6 having 20% poloxamer 407 and 0.2% HPMC K100 were optimized based on evaluation parameters. The gelation temperature of F4 and F6 was found to be 37°C ± 0.4 and 37°C ± 0.2, drug content 98.34 and 98.33% and drug release was 83.18, 82.4% in 4 hrs with a flux of 436.9 and 428.1 μg.cm2/hr, respectively. The release pattern of drug followed first-order kinetics with Higuchi release mechanism. The value of ‘n’ from Korsemeyer equation indicated the anomalous diffusional drug release. This study concluded that in situ gel enhanced the nasal residence time and thus may improve the bioavailability of the drug through nasal route by avoiding first pass metabolism Dhaka Univ. J. Pharm. Sci. 18(2): 183-193, 2019 (December)

scholarly journals Development and evaluation of in situ novel intragastric controlled-release formulation of hydrochlorothiazide

2011 ◽  
Vol 61 (1) ◽  
pp. 73-82 ◽  
Author(s):  
Ravikumar Patel ◽  
Jayvadan Patel
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
New Technology ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Release Formulation ◽  
Controlled Release Formulation ◽  
Rigid Mass ◽  
Formulation Factors

Development and evaluation of in situ novel intragastric controlled-release formulation of hydrochlorothiazide In situ forming intragastric controlled-release formulation is a new technology in the field of oral controlled-release delivery systems. The objective of this study was to develop formulations that can control drug release up to 24 hours. In addition, a combination of appropriate polymers and solvents was selected that could form a drug loaded gel at the process temperature of 60-70 °C, which gel could turn into a rigid mass upon exposure to dissolution fluid at body temperature. The drug release mechanism from this rigid mass was controlled by different formulation factors such as different polymer grades, polymer concentrations, hydrophobicity or hydrophilicity of solvents, different drug loadings, and physicochemical properties of additional excipients. After evaluating different formulation factors, Ethocel 10 FP and triethyl citrate were selected for further studies using hydrochlorothiazide as a model drug. Polynomial correlation between viscosity of the blank gel and drug release profile was also obtained.

DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Drug Release Mechanism ◽  
The Matrix ◽  
Gastro Retentive

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF IN SITU GEL OF XANTHAN GUM FOR OPHTHALMIC FORMULATION CONTAINING BRIMONIDINE TARTRATE

2018 ◽  
Vol 11 (7) ◽  
pp. 277 ◽  
Author(s):  
Vazir Ashfaq Ahmed ◽  
Divakar Goli
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Gelation Time ◽  
Gel Strength ◽  
Eye Drops ◽  
In Situ Gel ◽  
23 Factorial Design ◽  
Brimonidine Tartrate

Objective: The goal of this study was to develop and characterize an ion-activated in situ gel-forming brimonidine tartrate, solution eye drops containing xanthan gum as a mucoadhesive polymer.Method: Sol-gel formulation was prepared using gellan gum as an ion-activated gel-forming polymer, xanthan gum as mucoadhesive agent, and hydroxypropyl methyl cellulose (HPMC E50LV) as release retardant polymer. Phenylethyl alcohol is used as preservatives in borate buffer. The 23 factorial design was employed to optimize the formulation considering the concentration of gelrite, xanthan gum and HPMC as independent variables, gelation time, gel strength, and mucoadhesive force (N). Gelation time , gel strength, mucoadhesive force (N), viscosity (cP) and in vitro percentage drug release were chosen as dependent variables. The formulation was characteristics for pH, clarity, isotonicity, sterility, rheological behavior, and in vitro drug release, ocular irritation, and ocular visualization.Result: Based on desirability index of responses, the formulation containing a concentration of gelrite (0.4%), xanthan gum (0.21%), and HPMC (HPMC E50 (0.24%) was found to be the optimized formulation concentration developed by 23 factorial design. The solution eye drops resulted in an in situ phase change to gel-state when mixed with simulated tear fluid. The gel formation was also confirmed by viscoelastic measurements. Drug release from the gel followed non-fickian mechanism with 88% of drug released in 10 h, thus increased the residence time of the drug.Conclusion: An in situ gelling system is a valuable alternative to the conventional system with added benefits of sustained drug release which may ultimately result in improved patient compliance.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

scholarly journals DESIGN, OPTIMIZATION & IN-VITRO EVALUATION OF SODIUM ALGINATE BASED IN-SITU GEL OF RANITIDINE HYDROCHLORIDE IN ULCER TREATMENT

2021 ◽  
Vol 9 (1) ◽  
Author(s):  
Sanket Kumar ◽  
Mahesh Singh ◽  
Babulal Patel
Keyword(s):  
Peptic Ulcer ◽  
Drug Release ◽  
Sodium Alginate ◽  
Gelling Agent ◽  
Cross Linking ◽  
Physical Interaction ◽  
In Situ Gel ◽  
Ranitidine Hydrochloride ◽  
Ulcer Treatment

Peptic ulcer, it is the most common type of stomach disease, according to the American Gastroenterology Association. “We know that ulcers occur because there has been a disruption in the balance of factors that injure the digestive tract and those factors that protect it from injury,” The present investigation deal with the formulation, optimization and evaluation of sodium alginate based in situ gel of ranitidine hydrochloride (R-HCl) in ulcer treatment. The in-situ formulation are homogenous liquid when administration orally and become gel at the contact site. The evaluation of the formulation is dependent upon accurate results obtained by analytical method used during the study. Accurate results require the use of standard and a calibration procedure. Hence, standard plots of Ranitidine hydrochloride were prepared in (0.1N HCL, pH 1.2) solutions. Two, sodium alginate and calcium carbonate used as a polymer and cross-linking agent respectively in the formulation of in-situ gel. From the IR studies it may be concluded that the drug and carriers used undergo physical interaction there is no chemical change, and thus the gelling agent, cross-linking agent and other excipient is suitable for formulation of in-situ gel of ranitidine hydrochloride. Indicate that the formulation, DKF9 which was prepared by the Sodium alginate (2 gm) with Ranitidine Hydrochloride showed minimum drug release (sustained drug release) after 8 hrs. It can be concluded that the In-situ gel was beneficial for delivering the drug which needs sustained release to achieve the slow action. Keywords: In-situ gel, Peptic Ulcer, Ranitidine Hydrochloride (R-HCl), Sodium alginate.

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