scholarly journals Bioactive Multilayer Polylactide Films with Controlled Release Capacity of Gallic Acid Accomplished by Incorporating Electrospun Nanostructured Coatings and Interlayers

2019 ◽  
Vol 9 (3) ◽  
pp. 533 ◽  
Author(s):  
Luis Quiles-Carrillo ◽  
Nestor Montanes ◽  
José Lagaron ◽  
Rafael Balart ◽  
Sergio Torres-Giner
Keyword(s):  
Sustained Release ◽  
Gallic Acid ◽  
In Vitro Release ◽  
The Other ◽  
High Transparency ◽  
Release Capacity ◽  
Release Studies ◽  
Vitro Release ◽  
Saline Medium

The present research reports on the development of bi- and multilayer polylactide (PLA) films by the incorporation of electrospun nanostructured PLA coatings and interlayers containing the antioxidant gallic acid (GA) at 40 wt% onto cast-extruded PLA films. To achieve the bilayer structures, submicron GA-loaded PLA fibers were applied on 200-µm cast PLA films in the form of coatings by electrospinning for 1, 2, and 3 h. For the multilayers, the cast PLA films were first coated on one side by electrospinning, then sandwiched with 10-µm PLA film on the other side, and the resultant whole structure was finally thermally post-treated at 150 °C without pressure. Whereas the bilayer PLA films easily delaminated and lacked transparency, the multilayers showed sufficient adhesion between layers and high transparency for deposition times during electrospinning of up to 2 h. The incorporation of GA positively contributed to delaying the thermal degradation of PLA for approximately 10 °C, as all films were thermally stable up to 345 °C. The in vitro release studies performed in saline medium indicated that the GA released from the bilayer PLA films rapidly increased during the first 5 h of immersion while it stabilized after 45–250 h. Interestingly, the PLA multilayers offered a high sustained release of GA, having the capacity to deliver the bioactive for over 1000 h. In addition, in the whole tested period, the GA released from the PLA films retained most of its antioxidant functionality. Thus, during the first days, the bilayer PLA films can perform as potent vehicles to deliver GA while the multilayer PLA films are able to show a sustained release of the natural antioxidant for extended periods.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

scholarly journals Preparation and release characteristics study on the novel minocycline hydrochloride sustained-release capsule

2016 ◽  
Vol 11 ◽  
pp. S36-S42
Author(s):  
Songfeng Zhao ◽  
Xiao Zhang ◽  
Xiaojian Zhang ◽  
Xiuqin Shi ◽  
Jun Li ◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
The Novel ◽  
Promising Alternative ◽  
Release Studies ◽  
Reference Preparation ◽  
Minocycline Hydrochloride ◽  
Vitro Release ◽  
Extrusion Spheronization

In present study, a novel minocycline hydrochloride sustained-release capsule was prepared with the new extrusion-spheronization method. The in vitro release studies were performed using marketed sample as a reference and data were analyzed in terms of cumulative release amounts as a function of time. Results demonstrated that the developed analysis method was reliable and convenient for the quantification and dissolution study of minocycline hydrochloride. The release characteristics of different batches of preparations were quite similar with each other, similarity factors f2  of 12 batches were all within 50-100, and our developed sample was similar to reference preparation in release characteristics in vitro. The developed sustained-release preparation may be a promising alternative dosage form for treatment of related diseases. 

scholarly journals Pullulan: an advantageous natural polysaccharide excipient to formulate tablets of alendronate-loaded microparticles

2015 ◽  
Vol 51 (1) ◽  
pp. 27-33 ◽  
Author(s):  
Luana Mota Ferreira ◽  
Aline de Arce Velasquez ◽  
Scheila Rezende Schaffazick ◽  
Letícia Cruz
Keyword(s):  
Microcrystalline Cellulose ◽  
In Vitro Release ◽  
The Other ◽  
Average Weight ◽  
Direct Compression ◽  
Compression Force ◽  
Natural Polysaccharide ◽  
Release Studies ◽  
Vitro Release

This work reports the preparation of tablets by direct compression of sodium alendronate-loaded microparticles, using pullulan as filler. The tableting properties of pullulan were compared with those of microcrystalline cellulose and lactose. Pullulan tablets showed low variations in average weight, thickness and drug content. Moreover, these tablets exhibited a higher hardness compared to the other excipients. In vitro release studies showed that only pullulan was capable to maintain gastroresistance and release properties of microparticles, due to its ability to protect particles against damage caused by compression force. Thus, pullulan was considered an advantageous excipient to prepare tableted microparticles.

scholarly journals Formulation and Evaluation of Microsponge Based Nicorandil Sustained Released Tablet

2017 ◽  
Vol 9 (3) ◽  
pp. 285-296
Author(s):  
S. S. Patel ◽  
M. R. Patel ◽  
M. J. Patel
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Diffusion Method ◽  
P Value ◽  
Once Daily ◽  
Release Studies ◽  
Significant Difference ◽  
Vitro Release

The aim of the present work was to develop once-daily sustained release microsponges formulations of Nicorandil, a potent potassium channel opener used in cardiovascular diseases and it has low oral bioavailability (70%) and half-life 1 h. So, it is good candidate for sustained release formulations based on microsponge technology. The microsponges were prepared by using quasi-emulsion solvent diffusion method. Scanning Electron Microscopy (SEM) revealed that the microsponges of nicorandil with Eudragit - RSPO and HPMC K100M were smooth, porous, glossy and discrete spherical. The actual drug content and encapsulation efficiency of batch M1 to M9 were obtained in range of 62.05 ± 0.31 to 80.69 ± 0.43 and 64.41 ± 1.71 to 70.58 ± 1.12, respectively. The microsponges formulations were subjected to in-vitro release studies and the results were evaluated kinetically and statically. The best fitted model was found to be Korsmeyer - Peppas model (R2 = 0.9992) for M6 batch.  The ‘n’ value for Korsmeyer - Peppas model was between 0.5 and 1.0 which is indicative of non-Fickian diffusion. Statistical analysis using ANOVA yielded a p value of 0.572 for all the formulations, indicating that there was no significant difference among them.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin

2018 ◽  
Vol 11 (6) ◽  
pp. 4331-4337
Author(s):  
C Suja ◽  
Sismy C
Keyword(s):  
Sustained Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
Weight Variation ◽  
Sustained Release Tablets ◽  
Release Study ◽  
Vitro Release

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.

Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

1970 ◽  
Vol 1 (3) ◽  
pp. 257-266
Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Phenyl Acetic Acid ◽  
Solvent Evaporation Method ◽  
Elimination Half ◽  
Release Studies ◽  
Differential Scanning Colorimetry ◽  
Polymer Interactions ◽  
Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

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 Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia Catechu Extracts: Microencapsulation and In Vitro Release Study

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1655
Author(s):  
Zvezdelina Yaneva ◽  
Donika Ivanova ◽  
Nikolay Popov
Keyword(s):  
Composite System ◽  
Release Kinetics ◽  
Spectral Characteristics ◽  
In Vitro Release ◽  
Medium Ph ◽  
Release Capacity ◽  
Bioactive Substance ◽  
Acacia Catechu ◽  
Vitro Release

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

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