scholarly journals IN VITRO ENTRAPMENT AND RELEASE STUDIES OF LEVOFLOXACIN USING EPICHLOROHYDRIN-CROSSLINKED HYDROGEL

2019 ◽  
pp. 138-144
Author(s):  
ANGELI ANN S RESCOBER
Keyword(s):  
New Zealand ◽  
Drug Release ◽  
Release Rate ◽  
Drug Loading ◽  
Ophthalmic Solution ◽  
Antimicrobial Activities ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Polymer Ratio

Objective: This study aimed to optimize and evaluate the controlled release rate, ocular irritancy, and in vitro antimicrobial properties of levofloxacinentrapped in the epichlorohydrin-crosslinked hydrogel of sodium carboxymethyl cellulose (NaCMC) and gelatin.Materials and Methods: Various parameters such as polymer ratio, amount of crosslinker, temperature, reaction time, swelling capacity, and percentdrug loading were considered in Optimized levofloxacin hydrogel. Hydrogel preparations with higher amount of drug loaded were further analyzedto determine its in vitro drug release rate, ocular irritancy on New Zealand rabbits, and antimicrobial activities against Pseudomonas aeruginosaand Staphylococcus aureus. Optimized levofloxacin hydrogel (OLH) was then subjected to 3-month stability testing at 40 ± 2°C and 75 ± 5% relativehumidity in which samples were withdrawn at the end of each month for analysis.Results: Polymer groups with higher concentrations of NaCMC have higher swelling and drug loading capacities than those with higher gelatinconcentrations. Meanwhile, qualitative analysis using differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanningelectron microscopy verified the presence of levofloxacin in the epichlorohydrin-cross-linked hydrogel. Among the four polymer ratio, F3 was theoptimized hydrogel with drug-loaded concentration of 99.50%, which was within the acceptable assay limit of 0.5% levofloxacin solution based onUnited States Pharmacopeia monograph. It followed the Higuchi kinetic model with a drug release mechanism of super case 2 transport indicatinghydrogel swelling as a key factor for its controlled drug release. In vitro, antibacterial test against P. aeruginosa and S. aureus was sensitive to optimizedlevofloxacin hydrogel (OLH) with inhibitory diameter zones of 31.68 and 37.05 mm, respectively. Ocular irritancy test also showed that the OLH isnon-irritating on installation in the cul-de-sac of New Zealand rabbits.Conclusion: Optimized levofloxacin hydrogel was effective, non-irritating, and stable, which can be used as an alternative to conventional 0.5%levofloxacin ophthalmic solution.

scholarly journals Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres

2016 ◽  
Vol 19 (1) ◽  
pp. 58-67
Author(s):  
Paroma Arefin ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Order Release ◽  
Eudragit Rl ◽  
Fexofenadine Hcl

The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016

Release of Aspirin from Biodegradable Polyesterurethane Networks

2009 ◽  
Vol 79-82 ◽  
pp. 1431-1434 ◽  
Author(s):  
Ya Kai Feng ◽  
Shi Feng Zhang ◽  
Li Zhang ◽  
Jin Tang Guo ◽  
Yong Shen Xu
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Degradation Process ◽  
Crosslinking Density ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Model Drug ◽  
Phosphate Buffered Saline

In this paper, the release of model drug aspirin (ASP) from biodegradable polyesterurethane networks was studied. Poly(D,L-lactide-co-glycolide)urethane (PULG) networks were prepared from hydroxyl telechelic star-shaped oligo(D,L-lactide-co-glycolide) coupled with 1,6-diisocyanate-2,2,4-trimethylhexane and 1,6-diisocyanate-2,4,4-trimethylhexane or isophorone diisocyanate. PULG networks turned from transparent to opaque after ASP loading. PULG networks with lower crosslinking density always resulted in higher drug loaded content. The results of differential scanning calorimetry (DSC) and scanning electron microscope (SEM) measurements demonstrated that ASP was uniformly distributed in the networks. The drug release courses of ASP from PULG networks in phosphate buffered saline pH = 7.0 at 37 °C could be divided into three stages. Firstly, ASP release was at approximately uniform rate from PULG networks; Secondly, the release rate obviously increased for the degradation of the PULG networks; Thirdly, the release rate decreased gradually because most of the ASP had diffused out of the PULG networks. The crosslinking density of polyesterurethane networks also affected drug release rate. The in vitro release test revealed that ASP accelerated the degradation process of PULG, which exhibited a typical erosion-controlled release mechanism.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

scholarly journals 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

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
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.

Facile Synthesis of Chitosan Based-(AMPS-co-AA) Semi-IPNs as a Potential Drug Carrier: Enzymatic Degradation, Cytotoxicity, and Preliminary Safety Evaluation

2019 ◽  
Vol 16 (3) ◽  
pp. 242-253 ◽  
Author(s):  
Kaleem Ullah ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Haroon Rashid ◽  
Aamna Shah ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Cytotoxicity ◽  
Oral Drug ◽  
Specific Enzyme ◽  
Oral Toxicity ◽  
Scanning Calorimetry

Objective: The study describes the development of chitosan-based (AMPS-co-AA) semi-IPN hydrogels using free radical polymerization technique. Methods: The resulting hydrogels were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-Ray diffraction (XRD), and Scanning Electron Microscopy (SEM). The successful crosslinking of chitosan, 2- Acrylamido-2-Methylpropane Sulfonic Acid (AMPS), and Acrylic Acid (AA) was confirmed by FT IR. Unloaded and drug-loaded hydrogels exhibited higher thermal stability after crosslinking compared to the individual components. XRD confirmed the decrease in crystallinity after hydrogel formation and molecular dispersion of Oxaliplatin (OXP) in the polymeric network. SEM showed rough, vague and nebulous surface resulting from crosslinking and loading of OXP. Results: The experimental results revealed that swelling and drug release were influenced by the pH of the medium being low at acidic pH and higher at basic pH. Increasing the concentration of chitosan and AA enhanced the swelling, drug loading and drug release while AMPS was found to act inversely. Conclusion: It was confirmed that the hydrogels were degraded more by specific enzyme lysozyme as compared to the non-specific enzyme collagenase. In-vitro cytotoxicity suggested that the unloaded hydrogels were non-cytotoxic while crude drug and drug-loaded hydrogel exhibited dose-dependent cytotoxicity against HCT-116 and MCF-7. Results of acute oral toxicity on rabbits demonstrated that the hydrogels are non-toxic up to 3900 mg/kg after oral administration, as no toxicity or histopathological changes were observed in comparison to control rabbits. These pH-sensitive hydrogels appear to provide an ideal basis as a safe carrier for oral drug delivery.

scholarly journals Synthesis and Characterization of Lyophilized Chitosan-Based Hydrogels Cross-Linked with Benzaldehyde for Controlled Drug Release

2020 ◽  
Vol 2020 ◽  
pp. 1-10 ◽  
Author(s):  
Fouad Damiri ◽  
Yahya Bachra ◽  
Chaimaa Bounacir ◽  
Asmae Laaraibi ◽  
Mohammed Berrada
Keyword(s):  
Ascorbic Acid ◽  
Drug Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Tween 20 ◽  
Release Mechanism ◽  
Synthetic Process ◽  
Chitosan Salt

In this study, chitosan-based hydrogels were produced by incorporating three drugs with a different solubility into a polymer matrix. The lyophilized chitosan salt was prepared using an innovative and less-expensive synthetic process by the freeze-drying technique. Firstly, the three drugs (caffeine, ascorbic acid, and 5-fluorouracil (5-FU)) were selected as model drugs to test the in vitro release behavior of the hydrogel. The drugs were solubilized in chitosan salt, lyophilized, and cross-linked with benzaldehyde involving the formation of a Schiff base with (–C=N-) linkage to produce a physical hydrogel. Subsequently, the physicochemical properties of N-benzyl chitosan and lyophilized chitosan salt were evaluated by Fourier-transform infrared (FTIR) spectra, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The intrinsic viscosity of the conventional chitosan was determined by the Mark–Houwink–Sakurada equation. Moreover, the kinetics of hydrogel swelling and drug release were studied by the UV-visible method at physiological conditions (pH = 7.4 at 37°C). The results show that lyophilized N-benzyl chitosan had a maximum swelling ratio of 720 ± 2% by immersion in phosphate-buffered saline solutions (PBS) (pH = 7.4 at 37°C). In vitro drug releases were evaluated in PBS, and the obtained results show that the maximum drug release after 24 h was 42% for caffeine, 99% for 5-FU, and 94% for ascorbic acid. Then, to optimize the cumulative release of caffeine, Tween 20 was added and 98% as a release percentage was obtained. The drug-loading results were investigated with the Korsmeyer–Peppas kinetic model and applied to determine the drug release mechanism.

pH-Sensitive Interpenetrating Hydrogel for Eradication of Helicobacter pylori

2010 ◽  
Vol 3 (2) ◽  
pp. 924-932
Author(s):  
A K Gupta ◽  
Maurya S D ◽  
R C Dhakar ◽  
R D Singh
Keyword(s):  
Drug Release ◽  
Ph Value ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Crosslinking Process ◽  
Drug Entrapment Efficiency ◽  
Crosslinking Agents ◽  
Polymer Ratio

The interpenetrating hydrogels of clarithromycin were prepared by chemical crosslinking process using chitosan, poly (vinylpyrrolidone) and poly (acrylic acid) polymers and glutaraldehyde and N,N’-methylenebisacrylamide as crosslinking agents. The hydrogels were evaluated for FTIR analysis, differential scanning calorimetry (DSC), drug entrapment efficiency, scanning electron microscopy (SEM), swelling study, in-vitro drug release and mucoadhesive study. The formulation containing higher amount of chitosan showed greater swelling and drug release because of higher amount of NH2 as pendant group, which ionize at lower PH values. Finally, it was concluded that by appropriate modification of polymer ratio the extent of swelling and rate of drug release can be modulated. The result showed that IPN hydrogels prepared release the drug at lower PH value (PH 2.0) or in stomach thus maintaining antibiotic concentration in stomach for prolonged period of time.

scholarly journals Preparation and In vitro Evaluation of Theophylline Loaded Gastroretentive Floating Tablets of METHOCEL K4M

1970 ◽  
Vol 7 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Ferdous Khan ◽  
Md Shaikhul Millat Ibn Razzak ◽  
Md Ziaur Rahman Khan ◽  
Kazi Rashidul Azam ◽  
Sams Mohammad Anowar Sadat ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Lag Time ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Floating Tablets ◽  
Time Required

This investigation describes the preparation and in vitro evaluation of gastroretentive floating tablets of theophylline. Hydrophilic polymer METHOCEL K4M was used for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid), gel forming agent (METHOCEL K4M) and dose variation on drug release profile and floating properties were investigated. It has been observed that in all cases increase of the amount of floating agent caused a decrease of the floating lag time. Increase of theophylline load showed an increase of the floating lag time, which was independent of floating agent content. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixon-Crowell equations. The release rate, extent and mechanisms were found to be governed by the content of polymer and floating agent. The content of active ingredient was also a vital factor in controlling drug release pattern. It was found that polymer content and amount of floating agent significantly affected the time required for 50% of drug release (T50%), percentage drug release after 8 hours, release rate constant, and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was mainly dependent on presence of relative amount of theophylline, polymer and floating agent. Key words: Gastroretention, Floating tablet, Theophylline  DOI = 10.3329/dujps.v7i1.1220 Dhaka Univ. J. Pharm. Sci. 7(1): 65-70, 2008 (June)

scholarly journals Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

2015 ◽  
Vol 13 (2) ◽  
pp. 149-166 ◽  
Author(s):  
Navid Jubaer Ayon ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Sustained Release ◽  
Release Rate ◽  
Drug Loading ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Dissolution Apparatus

Polymeric microspheres of gliclazide were prepared to provide sustained release delivery of gliclazide to aid in continuous therapy with high margin of safety. Gliclazide was microencapsulated with different polymers namely HPMC K100LV, Ethocel (20 cps) and HPMC K100M by emulsion solvent evaporation technique using acetone as internal phase and liquid paraffin as external phase. Seventeen formulations were prepared using different drug loading and polymeric ratio of which nine formulations were prepared by a 32 full factorial design. Each formulation was evaluated for flow properties, particle size, surface morphology, drug entrapment efficiency, drug release and compatibility. Yield (%) for every batch of microspheres was measured. Flow properties of the microspheres were examined by determining bulk density, tapped density, Carr’s compressibility index, Hausner ratio and angle of repose. Particle size distribution was examined by sieving and particle size analyzer. Surface morphology was determined by scanning electron microscopy (SEM). In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) for a period of 8 hours at 37°C using phosphate buffer ( pH 7.4). FTIR and DSC studies established compatibility of the drug with the polymers. Microspheres prepared with Ethocel (20 cps) and HPMC K100M were free flowing than those prepared only with HPMC K100LV. Entrapment efficiencies were within 75.88-99.69%. Microspheres prepared with Ethocel (20 cps) and HPMC K100M showed more sustained release when compared to microspheres prepared with HPMC K100LV only. Increase in drug loading resulted in increased drug release for the microspheres. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranging from diffusion controlled to anomalous type. Ethocel and HPMC K100M in a ratio of 1:3 exhibited better sustained release properties than 1:1 and 3:1 ratios. The release rate of gliclazide from microspheres prepared with Ethocel (20 cps) and HPMC K100M was less than the release rate of gliclazide from microspheres prepared with HPMC K100LV, demonstrating Ethocel and HPMC K100M as suitable polymeric blend for preparing the controlled release formulation for gliclazide whereas, HPMC K100LV was found not suitable candidate when used alone as a polymer. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21893 Dhaka Univ. J. Pharm. Sci. 13(2): 149-166, 2014 (December)

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