Effect of drug loading extent on the in vitro release kinetic behaviour of nifedipine from polyacrylate microspheres

1990 ◽  
Vol 12 (3) ◽  
pp. 213-222 ◽  
Author(s):  
S. Benita ◽  
A. Barkai ◽  
Y.V. Pathak
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Release Kinetic ◽  
Kinetic Behaviour ◽  
Vitro Release

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 Cellulose/guar gum hydrogel microspheres as a magnetic anticancer drug carrier

BioResources ◽  
2019 ◽  
Vol 14 (2) ◽  
pp. 3615-3629 ◽  
Author(s):  
Yanli Li ◽  
Yucheng Feng ◽  
Jun Jing ◽  
Fei Yang
Keyword(s):  
Anticancer Drug ◽  
Guar Gum ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Adsorption Effect ◽  
Magnetic Hydrogel ◽  
Vitro Release ◽  
Hydrogel Microspheres

A novel magnetic anticancer drug carrier based on cellulose, guar gum, and Fe3O4 hydrogel microspheres was synthesized by chemical crosslinking. These microspheres were crosslinked with epoxy chloropropane and loaded with 5-fluorouracil (5-fu). The effect of the ratio of cellulose to guar gum on bead size, drug loading, and in vitro release behaviors were investigated. The influence of the magnetic content on drug loading and in vitro release behaviors were also evaluated. The magnetic hydrogel microspheres were characterized via an optical microscope, Fourier transform infrared spectroscopy, swelling behavior analysis, vibrating sample magnetometer, and ultraviolet absorption spectroscopy. The results showed that as the ratio of cellulose to guar gum increased from 3:1 to 5:1, the particle size increased from 395 to 459 um. Moreover, the drug loading capacity, encapsulation efficiency, and in vitro release behavior were influenced by the ratio of cellulose/guar gum and Fe3O4 content. Finally, the Fe3O4 particle had an adsorption effect on the drug, thereby reducing the maximum cumulative release.

Calcium phosphate porous pellets as drug delivery systems: Effect of drug carrier composition on drug loading and in vitro release

2012 ◽  
Vol 32 (11) ◽  
pp. 2679-2690 ◽  
Author(s):  
Hiva Baradari ◽  
Chantal Damia ◽  
Maggy Dutreih-Colas ◽  
Etienne Laborde ◽  
Nathalie Pécout ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Calcium Phosphate ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Vitro Release

scholarly journals Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4707
Author(s):  
Maria Camilla Bergonzi ◽  
Marzia Vasarri ◽  
Giulia Marroncini ◽  
Emanuela Barletta ◽  
Donatella Degl’Innocenti
Keyword(s):  
Cell Migration ◽  
Load Capacity ◽  
Drug Loading ◽  
Neuroblastoma Cell ◽  
In Vitro Release ◽  
Human Neuroblastoma Cell ◽  
Prolonged Release ◽  
Human Neuroblastoma ◽  
Vitro Release

Thymoquinone (TQ) is the main active ingredient of Nigella sativa essential oil, with remarkable anti-neoplastic activities with anti-invasive and anti-migratory abilities on a variety of cancer cell lines. However, its poor water solubility, high instability in aqueous solution and pharmacokinetic drawbacks limits its use in therapy. Soluplus® and Solutol® HS15 were employed as amphiphilic polymers for developing polymeric micelles (SSM). Chemical and physical characterization studies of micelles are reported, in terms of size, homogeneity, zeta potential, critical micelle concentration (CMC), cloud point, encapsulation efficiency (EE%), load capacity (DL), in vitro release, and stability. This study reports for the first time the anti-migratory activity of TQ and TQ loaded in SSM (TQ-SSM) in the SH-SY5Y human neuroblastoma cell line. The inhibitory effect was assessed by the wound-healing assay and compared with that of the unformulated TQ. The optimal TQ-SSM were provided with small size (56.71 ± 1.41 nm) and spherical shape at ratio of 1:4 (Soluplus:Solutol HS15), thus increasing the solubility of about 10-fold in water. The entrapment efficiency and drug loading were 92.4 ± 1.6% and 4.68 ± 0.12, respectively, and the colloidal dispersion are stable during storage for a period of 40 days. The TQ-SSM were also lyophilized to obtain a more workable product and with increased stability. In vitro release study indicated a prolonged release of TQ. In conclusion, the formulation of TQ into SSM allows a bio-enhancement of TQ anti-migration activity, suggesting that TQ-SSM is a better candidate than unformulated TQ to inhibit human SH-SY5Y neuroblastoma cell migration.

scholarly journals FABRICATION OF BIOADHESIVE OCUSERT WITH DIFFERENT POLYMERS: ONCE A DAY DOSE

2018 ◽  
Vol 10 (6) ◽  
pp. 309
Author(s):  
Aya M. Dawaba ◽  
Hamdy M. Dawaba ◽  
Amal S. M. Abu El-enin ◽  
Maha K. A. Khalifa
Keyword(s):  
In Vitro Release ◽  
Methyl Cellulose ◽  
Storage Period ◽  
Poly Vinyl Alcohol ◽  
Release Kinetic ◽  
Casting Technique ◽  
Process Characterization ◽  
Vitro Release

Objective: The objective of this current study is to fabricate ocuserts to control the drug release from chosen bioadhesive polymeric matrixes to enhance patient compliance. Ciprofloxacin HCl (CFX HCl) was selected as a model drug.Methods: Different bioadhesive polymers with different film forming capabilities namely Hydroxy Propyl Methyl Cellulose (HPMC K4M), Poly Vinyl Alcohol (PVA), Sodium Carboxy Methyl Cellulose (Na CMC), Hydroxy Propyl Cellulose (HPC), Sodium Alginate (Na Alg.), pullulan and Xanthan Gum (XG) in different ratios were used in fabricating ocuserts using solvent-casting technique. Propylene Glycol (PG) was used as a plasticizer to facilitate the fabrication process. Characterization tests of the developed ocuserts were performed as well as bioadhesive tests and in vitro release studies of the incorporated drug. The obtained results were analysed using different release kinetic models. Stability of the selected ocuserts was investigated at 40±0.5 °C and 75±5% Relative Humidity (RH) for three months’ storage period. In vivo ocular irritation test was performed to investigate the safety of the formula in rabbits’ eyes as well as to test the release profile and thus to estimate In vitro In vivo correlation.Results: All the prepared ocuserts showed the uniformity of film characterization and bioadhesion strength ranged from 240±66 and 158±52dyne/cm2. Selected formula from the in vitro release study tested for in vivo study showed the slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In vitro In vivo correlation showed an excellent correlation with R2 value of 0.9982.Conclusion: PVA based ocuserts proven to be a promising once-daily, effective and safe ocular delivery system of the drug.

scholarly journals Study on the influence of technological factors on drug loading of poorly water-soluble drug on MCM-41 mesoporous carrier

Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 351-356
Author(s):  
Teodora Popova ◽  
Christina Voycheva ◽  
Borislav Tzankov
Keyword(s):  
Loading Rate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Water Soluble ◽  
Technological Factors ◽  
Loading Process ◽  
Water Soluble Drug ◽  
Vitro Release ◽  
Mcm 41

The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained.

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