Sinomenine-loaded microcapsules fabricated by phase reversion emulsification-drying in liquid method: An evaluation of process parameters, characterization, and released properties

2017 ◽  
Vol 33 (4) ◽  
pp. 382-396 ◽  
Author(s):  
Wen Zhang ◽  
Yan Gao ◽  
Ning Yang ◽  
Hua Zhang ◽  
Feng Zhang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Drug Loading ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Fickian Diffusion ◽  
Anti Cancer ◽  
Methyl Thiazolyl Tetrazolium Assay ◽  
Natural Alkaloid

Sinomenine is a natural alkaloid with important biological activities (e.g. anti-cancer, anti-inflammatory, and anti-allergic). However, the unstability and short half-life absolutely limited its application to foods. Microencapsulation technology can offer a way to solve these issues. In this study, polylactic acid microcapsules loading sinomenine hydrochloride were fabricated by phase inversion emulsification-drying in liquid technique. The results showed that microcapsules had nice spherical shape, uniform particle size, and free flowing. The encapsulation efficiency was 89.2% and drug loading was 8.9% under the optimal conditions. In vitro release assays demonstrated that release of sinomenine from microcapsules was sustained and slow. Moreover, it was found that the sinomenine release fitted Fickian diffusion mechanism. The results of cytotoxicity study showed that sinomenine-loaded microcapsules were biocompatible. Sinomenine-loaded microcapsules could inhibit the growth of MDA-MB-231 cells using methyl thiazolyl tetrazolium assay. In summary, polylactide microcapsules exhibit excellent properties for sinomenine that can be used in drug or food industry.

scholarly journals Three-Dimensionally Ordered Macroporous-Mesoporous Bioactive Glass Ceramics for Drug Delivery Capacity and Evaluation of Drug Release

2020 ◽  
Author(s):  
Reedwan Bin Zafar Auniq ◽  
Namon Hirun ◽  
Upsorn Boonyang
Keyword(s):  
Drug Release ◽  
Bioactive Glass ◽  
Drug Loading ◽  
Diffusion Mechanism ◽  
Sol Gel ◽  
Glass Ceramics ◽  
Fickian Diffusion ◽  
Ordered Macroporous ◽  
Mesoporous Bioactive Glass

Bioactive glass ceramics (BGCs) have been used in orthopedic and dentistry due to having better osteoconductive and osteostimulative properties. This study aimed to evaluate and compare the drug release properties of two different BGCs; 45S5 and S53P4. The BGCs were composed with four phases of SiO2 – CaO – Na2O – P2O5 system, synthesized by sol–gel method using dual templates; a block-copolymer as mesoporous templates and polymer colloidal crystals as macroporous templates, called three-dimensionally ordered macroporous-mesoporous bioactive glass ceramics (3DOM-MBGCs). In vitro bioactivity test performed by soaking the 3DOM-MBGCs in simulated body fluid (SBF) at 37°C. The results indicated that, the 45S5 have the ability to grow hydroxyapatite-like layer on the surfaces faster than S53P4. Gentamicin drug was used to examine in vitro drug release properties in phosphate buffer solution (PBS). The amount of drug release was quantified through UV/Vis spectroscopy by using o-phthaldialdehyde reagent. S53P4 showed high drug loading content. The outcome of drug release in PBS showed that both S53P4 and 45S5 exhibited a slowly continuous gentamicin release. The resultant drug release profiles were fitted to the Peppas-Korsmeyer model to establish the predominant drug release mechanisms, which revealed that the kinetics of drug release from the glasses mostly dominated by Fickian diffusion mechanism.

EFFECT OF HYDROPHILIC POLYMERS ON CONTROLLED RELEASE MATRIX TABLETS OF ACYCLOVIR

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (01) ◽  
pp. 42-49
Author(s):  
P Ashok Kumar ◽  
◽  
S. Damodar Kumar
Keyword(s):  
Controlled Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Fickian Diffusion ◽  
Sem Images ◽  
Weight Variation ◽  
Karaya Gum

Acyclovir was formulated as oral controlled release matrix tablets using natural and synthetic polymers separately or in combinations. Tablets were prepared by direct compression method. The tablets were evaluated to thickness, weight variation test, drug content, hardness, friability and in vitro release studies.All the formulations showed compliance with pharmacopoeal standards. The tablets prepared with various combination of hydroxy propyl methylcellulose (HPMC K100), locust bean gum (LBG) and karaya gum (KG) failed to produce the desired controlled release. Dissolution studies indicated that formulation F5 was most successful of the study. The formulation F5 exhibited anomalous (non-Fickian) diffusion mechanism. Based on the results of in-vitro studies it was concluded that the hydrophilic polymers canbe used as an effective matrix former to provide controlled release of acyclovir. SEM images of tablet after dissolution showed pore formation. FT-IR and DSC study did not show any possibility of interaction between acyclovir and excipients.

Hollow Mesoporous Spheres with Cubic Pore Network as a Potential Carrier for Drug Storage and its In Vitro Release Kinetics

2005 ◽  
Vol 20 (1) ◽  
pp. 54-61 ◽  
Author(s):  
Yu-Fang Zhu ◽  
Jian-Lin Shi ◽  
Yong-Sheng Li ◽  
Hang-Rong Chen ◽  
Wei-Hua Shen ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Pore Network ◽  
Fickian Diffusion ◽  
Step Method ◽  
Release Process ◽  
Drug Molecules ◽  
Mcm 41

The hollow mesoporous spheres (HMS) with cubic pore network have been synthesized via a simple two-step method. Two drugs of different molecules size, Aspirin and Gentamicin, were tested by one simple adsorption process. Up to 336 mg Aspirin molecules can be stored in 1.0 g HMS, while Gentamicin molecules of much larger size are much more difficult to be introduced into the pore channels of HMS. The same results can be obtained by using MCM-48 and MCM-41 as comparative mesoporous carriers. The HMS shows significantly higher storage amount of Aspirin than conventional MCM-48 and MCM-41 due to its hollow core structure. The release process of HMS-Aspirin, MCM-48-Aspirin and MCM-41-Aspirin are found to have a sustained-release property and follow a Fickian diffusion mechanism. Moreover, the HMS is suitable for storage of drug molecules of much smaller size.

scholarly journals Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1021
Author(s):  
Cristiane M. Pinto ◽  
Laila S. Horta ◽  
Amanda P. Soares ◽  
Bárbara A. Carvalho ◽  
Enio Ferreira ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Average Diameter ◽  
Controlled Drug Release ◽  
High Drug ◽  
Inflammatory Parameters ◽  
High Interaction ◽  
Ulcerative Lesions

Doxorubicin (DOX), a chemotherapy drug successfully used in the therapy of various types of cancer, is currently associated with the mucositis development, an inflammation that can cause ulcerative lesions in the mucosa of the gastrointestinal tract, abdominal pain and secondary infections. To increase the safety of the chemotherapy, we loaded DOX into nanostructured lipid carriers (NLCs). The NLC–DOX was characterized by HPLC, DLS, NTA, Zeta potential, FTIR, DSC, TEM and cryogenic-TEM. The ability of NLC–DOX to control the DOX release was evaluated through in vitro release studies. Moreover, the effect of NLC–DOX on intestinal mucosa was compared to a free DOX solution in C57BL/6 mice. The NLC–DOX showed spherical shape, high drug encapsulation efficiency (84.8 ± 4.6%), high drug loading (55.2 ± 3.4 mg/g) and low average diameter (66.0–78.8 nm). The DSC and FTIR analyses showed high interaction between the NLC components, resulting in controlled drug release. Treatment with NLC–DOX attenuated DOX-induced mucositis in mice, improving shortening on villus height and crypt depth, decreased inflammatory parameters, preserved intestinal permeability and increased expression of tight junctions (ZO-1 and Ocludin). These results indicated that encapsulation of DOX in NLCs is viable and reduces the drug toxicity to mucosal structures.

Design of atrazine containing polysaccharide based slow release formulations to control environmental hazards

2017 ◽  
Vol 1 (1) ◽  
Author(s):  
Baljit Singh ◽  
Devender Kumar Sharma ◽  
Abhishek Dhiman
Keyword(s):  
Slow Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Health Concern ◽  
Natural Polysaccharide ◽  
Scanning Electron Micrography ◽  
Controlled Release Formulations ◽  
Swelling Studies

Atrazine is more reliable, flexible, effective and less expensive herbicide than any other available weed control approaches. However, easy leaching of atrazine is a matter of great environmental and health concern which limits its strong recommendation for practical applicability. Hence, controlled release formulations of atrazine, specially based on natural polysaccharide, are required for delivery and resolve the problems associated with conventional formulations. In the present work, slow release atrazine containing alginate-agar based bead formulations have been prepared and characterized by scanning electron micrography, Fourier transform infrared spectroscopy and swelling studies. The release of atrazine from the beads occurred through non-Fickian diffusion mechanism. The release of atrazine from the beads in the soil has been observed slower and lesser in soil as compared to the in vitro release. Besides providing the slow release of atrazine, these formulations after degradation may enhance the fertility of the soil.

scholarly journals Preparation and Characterization of Aminoglycoside-Loaded Chitosan/Tripolyphosphate/Alginate Microspheres against E. coli

Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3326
Author(s):  
Estefanía Tiburcio ◽  
Eduardo García-Junceda ◽  
Leoncio Garrido ◽  
Alfonso Fernández-Mayoralas ◽  
Julia Revuelta ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Bacterial Resistance ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Antibacterial Properties ◽  
Fickian Diffusion ◽  
Burst Release ◽  
E Coli ◽  
Gel Beads

Although aminoglycosides are one of the common classes of antibiotics that have been widely used for treating infections caused by pathogenic bacteria, the evolution of bacterial resistance mechanisms and their inherent toxicity have diminished their applicability. Biocompatible carrier systems can help sustain and control the delivery of antibacterial compounds while reducing the chances of antibacterial resistance or accumulation in unwanted tissues. In this study, novel chitosan gel beads were synthesized by a double ionic co-crosslinking mechanism. Tripolyphosphate and alginate, a polysaccharide obtained from marine brown algae, were employed as ionic cross-linkers to prepare the chitosan-based networks of gel beads. The in vitro release of streptomycin and kanamycin A was bimodal; an initial burst release was observed followed by a diffusion mediated sustained release, based on a Fickian diffusion mechanism. Finally, in terms of antibacterial properties, the particles resulted in growth inhibition of Gram-negative (E. coli) bacteria.

scholarly journals Cubosomes Dispersions as Enhanced Indomethacin Oral Delivery Systems: In vitro and Stability Evaluation

2021 ◽  
pp. 24-35
Author(s):  
Iman M. Alfagih ◽  
Bushra AlQuadeib ◽  
Basmah Aldosari ◽  
Alanood Almurshedi ◽  
Mohamed M. Badran ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Poloxamer 407 ◽  
Fickian Diffusion ◽  
The Stability ◽  
Oral Delivery Systems ◽  
Kinetics Of

Aims: To improve the dissolution of indomethacin through developing liquid indomethacin loaded cubosomes dispersion for oral delivery. Methodology: Glyceryl monooleate based indomethacin loaded cubosomes dispersion were prepared using Taguchi design to study the effect of indomethacin to the disperse phase ratio and poloxamer 407 (PLX%) concentrations on the particle size and entrapment efficiency (%EE). Furthermore, in vitro release in phosphate buffer (pH 6.8), and morphology were investigated. Also, the stability of indomethacin loaded cubosomes dispersions was examined after 6 months storage at 25°C in the dark. Results: The prepared indomethacin cubosomes dispersions were in the nanoscale (184.53±0.7 to 261.33±0.8 nm) with reasonable %EE (49.30±2.6 to 95.55±3.4 %). Moreover, a biphasic release profile was predominant for all formulations, up to 50% of payload released after 2h followed by a second continuous sustained release phase over 24h. The kinetics of indomethacin release was best explained by Higuchi model and the mechanism of drug release from these cubosomes dispersions was by fickian diffusion mechanism. In general, the indomethacin loaded cubosomes dispersions were stable after 6 months storage at 25°C in the dark. Conclusion: Indomethacin loaded cubosomes dispersions proved to be a successful platform to encapsulate and enhance the release of indomethacin with a good stability profile over 6 months.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

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.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Sign in / Sign up

Export Citation Format

Share Document