Prednisolone Loaded Tamarind Gum Microspheres for Colonic Delivery

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i56b33959 ◽

2021 ◽

pp. 324-332

Author(s):

Harish K. Kunjwani ◽

Dinesh M. Sakarkar

Keyword(s):

Drug Release ◽

Controlled Drug Release ◽

Local Concentration ◽

Colonic Delivery ◽

Simulated Environment ◽

S 100 ◽

Long Time ◽

Sensitive Property ◽

Microsphere Preparation

The aim of this work was to formulate a novel multiparticulate system having pH sensitive property and specific enzyme biodegradability for colon specific drug delivery of Prednisolone (PD). Natural polysaccharide, Tamarind gum is used for microsphere preparation and Eudratit S- 100 for coating to provide pH controlled drug release. The formulation aims at minimal degradation and optimum delivery of the drug with relatively higher local concentration, which may provide more effective therapy for inflammatory bowel disease including Crohn disease and ulcerative colitis. Tamarind gum microspheres were prepared by emulsion dehydration technique using polymer in ratio of 1:1 to 1: 9. These microspheres were coated with Eudragit S-100 by oil in oil solvent evaporation method using core: coat ration (5:1). Tamarind gum microspheres and Eudragit coated tamarind gum microspheres were evaluated for surface morphology, particle size and size distribution, percentage drug entrapment, surface accumulation studies, in vitro drug release in simulated gastrointestinal fluids. The effect of various formulation variables were studied the prepared microspheres were spherical in shape in the size range of 64 µm to 113 µm, the encapsulation efficiency was in range of 30-72% depending upon the concentration of gum. The drug release was about 14-20% in first four hours of study gradually rises in 5th hour and 85% drug release occurs in 10-12% hr thus showing desirable drug release in the colonic simulated environment. PD tamarind gum microspheres are thought to have the potential to maintain drug concentration within target ranges for a long time, decreasing the side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency. The animal study done using acetic acid induced colitis model on rats also suggest the anti inflammatory activity of the formulation.

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Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

Acta Pharmaceutica ◽

10.2478/v10007-012-0034-x ◽

2012 ◽

Vol 62 (4) ◽

pp. 529-545 ◽

Cited By ~ 23

Author(s):

Anuj Chawla ◽

Pooja Sharma ◽

Pravin Pawar

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Naproxen Sodium ◽

Drug Loading ◽

Size Analysis ◽

Scanning Calorimetry ◽

Sem Images ◽

S 100 ◽

Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

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Organic-Inorganic Hybrid Hollow Mesoporous Organosilica Nanoparticles for Efficient Ultrasound-Based Imaging and Controlled Drug Release

Journal of Nanomaterials ◽

10.1155/2014/972475 ◽

2014 ◽

Vol 2014 ◽

pp. 1-8 ◽

Cited By ~ 18

Author(s):

Xiaoqin Qian ◽

Wenping Wang ◽

Wentao Kong ◽

Yu Chen

Keyword(s):

Drug Release ◽

Ultrasound Irradiation ◽

Controlled Drug Release ◽

Inorganic Hybrid ◽

Templating Method ◽

Anticancer Drug Delivery ◽

Cavitation Effect ◽

Contrast Enhanced

A novel anticancer drug delivery system with contrast-enhanced ultrasound-imaging performance was synthesized by a typical hard-templating method using monodispersed silica nanoparticles as the templates, which was based on unique molecularly organic/inorganic hybrid hollow periodic mesoporous organosilicas (HPMOs). The highly dispersed HPMOs show the uniform spherical morphology, large hollow interior, and well-defined mesoporous structures, which are very beneficial for ultrasound-based theranostics. The obtained HPMOs exhibit excellent performances in contrast-enhanced ultrasonography bothin vitroandin vivoand can be used for the real-time determination of the progress of lesion tissues during the chemotherapeutic process. Importantly, hydrophobic paclitaxel- (PTX-) loaded HPMOs combined with ultrasound irradiation show fast ultrasound responsiveness for controlled drug release and higherin vitroandin vivotumor inhibition rates compared with free PTX and PTX-loaded HPMOs, which is due to the enhanced ultrasound-triggered drug release and ultrasound-induced cavitation effect. Therefore, the achieved novel HPMOs-based nanoparticle systems will find broad application potentials in clinically ultrasound-based imaging and auxiliary tumor chemotherapy.

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FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39965 ◽

2021 ◽

pp. 206-215

Author(s):

DHARMENDER PALLERLA ◽

SUMAN BANOTH ◽

SUNKARI JYOTHI

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Controlled Drug Release ◽

Fickian Diffusion ◽

Simulated Gastric Fluid ◽

Release Mechanism ◽

Release Studies ◽

Swelling Studies ◽

Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

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Design, Development, and Optimization of Polymeric Based-Colonic Drug Delivery System of Naproxen

The Scientific World JOURNAL ◽

10.1155/2013/654829 ◽

2013 ◽

Vol 2013 ◽

pp. 1-12 ◽

Cited By ~ 5

Author(s):

Pooja Sharma ◽

Anuj Chawla ◽

Pravin Pawar

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Ph Sensitive ◽

Time Dependent ◽

Wet Granulation ◽

Design Development ◽

Caecal Content ◽

S 100 ◽

Eudragit S 100

The aim of present investigation deals with the development of time-dependent and pH sensitive press-coated tablets for colon specific drug delivery of naproxen. The core tablets were prepared by wet granulation method then press coated with hydroxypropyl cellulose (HPC) or Eudragit RSPO : RLPO mixture and further coated with Eudragit S-100 by dip immerse method. Thein vitrodrug release study was conducted in different dissolution media such as pH 1.2, 6.8, and 7.4 with or without rat caecal content to simulate GIT conditions. Surface morphology and cross-sectional view of the tablets were visualized by scanning electron microscopy (SEM). All prepared batches were in compliance with the pharmacopoeial standards. The tablets which are compression coated with HPC followed by Eudragit S-100 coated showed highestin vitrodrug release of 98.10% in presence of rat caecal content. The SEM of tablets suggested that the number of pores got increased in pH 7.4 medium followed by dissolution of coating layer. The tablets coat erosion study suggested that the lag time depends upon the coating concentrations of polymers. A time-dependent hydrophilic polymer and pH sensitive polymer based press-coated tablets of naproxen were promising delivery for colon targeting.

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DESIGN AND EVALUATION OF EUDRAGIT COATED LOSARTAN POTASSIUM CONTROLLED RELEASE PELLETS BY PAN COATING TECHNIQUE

INDIAN DRUGS ◽

10.53879/id.50.10.p0030 ◽

2013 ◽

Vol 50 (10) ◽

pp. 30-38

Author(s):

S Vidyadhara ◽

◽

R. L. C. Sasidhar ◽

P Thrilochani ◽

L. K. Lavanya

Keyword(s):

Controlled Release ◽

Drug Release ◽

Methyl Cellulose ◽

Losartan Potassium ◽

Scanning Calorimetry ◽

Coating Agent ◽

Coating Technique ◽

S 100 ◽

Eudragit S 100

The present investigation was focused on the development and evaluation of controlled release pellets of losartan potassium with Eudragit S 100 and hydroxypropyl methyl cellulose phthalate (HPMCP) by employing pan coating technique. Eudragit S 100, a high viscosity grade controlled release polymer, was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I. pH conditions. The prepared pellets were evaluated for particle size, drug content, friability and for in vitro drug release. The formulations were further characterized to identify any possible interactions by FTIR spectroscopy and differential scanning calorimetry. The surface morphology of the pellets was studied by scanning electron microscopy. From the results it was observed that due to increase in the concentration of Eudragit the drug release was extended up to 12 hours. The increase in the HPMCP polymeric concentration in formulations showed initial delay in drug release.

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In Vitro and In Vivo Biocompatibility of Novel Zwitterionic Poly(Beta Amino)Ester Hydrogels Based on Diacrylate and Glycine for Site‐Specific Controlled Drug Release

Macromolecular Chemistry and Physics ◽

10.1002/macp.201900188 ◽

2019 ◽

Vol 220 (17) ◽

pp. 1900188

Author(s):

Vuk V. Filipović ◽

Marija M. Babić ◽

Dejan Gođevac ◽

Aleksandar Pavić ◽

Jasmina Nikodinović‐Runić ◽

...

Keyword(s):

Drug Release ◽

Controlled Drug Release ◽

Amino Ester ◽

Site Specific

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A combined low-frequency electromagnetic and fluidic stimulation for a controlled drug release from superparamagnetic calcium phosphate nanoparticles: potential application for cardiovascular diseases

Journal of The Royal Society Interface ◽

10.1098/rsif.2018.0236 ◽

2018 ◽

Vol 15 (144) ◽

pp. 20180236 ◽

Cited By ~ 8

Author(s):

Alessandra Marrella ◽

Michele Iafisco ◽

Alessio Adamiano ◽

Stefano Rossi ◽

Maurizio Aiello ◽

...

Keyword(s):

Drug Delivery ◽

Animal Model ◽

Cardiovascular Diseases ◽

Drug Release ◽

Biological Effects ◽

Low Frequency ◽

Controlled Drug Release ◽

Drug Dose

Alternative drug delivery approaches to treat cardiovascular diseases are currently under intense investigation. In this domain, the possibility to target the heart and tailor the amount of drug dose by using a combination of magnetic nanoparticles (NPs) and electromagnetic devices is a fascinating approach. Here, an electromagnetic device based on Helmholtz coils was generated for the application of low-frequency magnetic stimulations to manage drug release from biocompatible superparamagnetic Fe-hydroxyapatite NPs (FeHAs). Integrated with a fluidic circuit mimicking the flow of the cardiovascular environment, the device was efficient to trigger the release of a model drug (ibuprofen) from FeHAs as a function of the applied frequencies. Furthermore, the biological effects on the cardiac system of the identified electromagnetic exposure were assessed in vitro and in vivo by acute stimulation of isolated adult cardiomyocytes and in an animal model. The cardio-compatibility of FeHAs was also assessed in vitro and in an animal model. No alterations of cardiac electrophysiological properties were observed in both cases, providing the evidence that the combination of low-frequency magnetic stimulations and FeHAs might represent a promising strategy for controlled drug delivery to the failing heart.

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Pseudolatex from STR 5L Block Rubber for Drug Delivery

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.844.166 ◽

2013 ◽

Vol 844 ◽

pp. 166-169 ◽

Cited By ~ 1

Author(s):

Prapaporn Boonme ◽

Kamon Panrat ◽

Wiwat Pichayakorn

Keyword(s):

Drug Release ◽

Contact Allergy ◽

Drug Loading ◽

Methyl Cellulose ◽

Controlled Drug Release ◽

Colloidal Dispersion ◽

Mineral Oil ◽

Lauryl Sulfate ◽

Drug Encapsulation

Pseudolatex is colloidal dispersion containing spherical solid or semisolid particles and can be prepared from any existing thermoplastic water-insoluble polymers. It is useful for drug encapsulation and controlled drug release. In this study, pseudolatex base was prepared from STR 5L block rubber. The various parameters such as speed and time of homogenization, type and concentration of surfactants, amount of mineral oil, and type of drug loading were studied to prepare the stable pseudolatex. These preparations were evaluated in particle size, pH, viscosity, emulsion stability, drug encapsulation, and in vitro drug release. It was found that the most stable formulation contained 3.5% block rubber, 0.2% methyl cellulose, 6% mineral oil, 4% dibutyl phthalate, 2% sodium lauryl sulfate, and 2% Uniphen P-23 using the speed and time of homogenizer as 20000 rpm and 20 minutes, respectively. Furthermore, the pseudolatex bases reduced the protein impurity form 0.5516% to 0.2108% in formulation with mineral oil and to 0.1781% in formulation without mineral oil, that could decrease contact allergy caused by the protein allergens. Dichloromethane residues in pseudolatex bases were 22.05 mg/L and 7.85 mg/L in formulations with and without mineral oil, respectively, that were satisfied from USP recommendation value of lower than 600 mg/L. Propranolol HCl, lidocaine HCl, and indomethacin could be loaded into pseudolatex only in the concentration of 1%. However, lidocaine base in the concentration of 1-5% could be loaded into pseudolatex which had the similar physical properties and stability to pseudolatex base. The in vitro drug release from pseudolatexs provided the controlled drug release for more than 24 hr.

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Bioinspired nanocarriers for an effective chemotherapy of hepatocellular carcinoma

Journal of Biomaterials Applications ◽

10.1177/0885328218772721 ◽

2018 ◽

Vol 33 (1) ◽

pp. 72-81 ◽

Cited By ~ 5

Author(s):

Lei Xu ◽

Shuo Wu ◽

Xiaoqiu Zhou

Keyword(s):

Hepg2 Cells ◽

Blood Circulation ◽

Antitumor Effect ◽

Membrane Vesicles ◽

Controlled Drug Release ◽

Coated Nanoparticles ◽

Rbc Membrane ◽

Long Time

Drug-loaded nanoparticles have been widely researched in the antitumor. However, some of them are unsatisfactory in the long blood circulation and controlled drug release. Red blood cell (RBC) membrane vesicles (RV)-coated nanoparticles have gained more and more attention in drug delivery for their many unique advantages, such as excellent stability, long blood circulation, and reduced the macrophage cells uptake. Herein, by utilizing the advantages of RV, we fabricated RV-coated poly(lactide- co-glycolide) (PLGA)–docetaxel (RV/PLGA/DTX) nanoparticles to enhance the antitumor efficiency in vivo. The RV/PLGA/DTX showed spherical morphology with particle size of about 100 nm and zeta potential at −12.63 mV, which could maintain stability for a long time. The RV/PLGA/DTX significantly enhanced cellular uptake of DTX compared to PLGA/DTX in HepG2 cells. Moreover, RV/PLGA/DTX showed the strongest antitumor effect in vitro. Prolonged blood circulation and enhanced DTX accumulation at the tumor site through enhanced permeability and retention (EPR) effect were achieved by RV/PLGA/DTX, which eventually obtained satisfactory antitumor effect and depressed system toxicity on mice bearing HepG2 xenografts mouse models when compared with free DTX. The hematoxylin and eosin (H&E) and immunofluorescence assays further proved the advantages of RV/PLGA/DTX in vivo antitumor. These RV-coated nanoparticles provide a mimetic therapy, completely inhibited the growth of the HepG2 cells, and with simple compositions, suggesting it to be an ideal strategy for improving the antitumor effect of drug-loaded nanoparticles.

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