Trigonelline hydrochloride conjugated onto PEGylated nanodiamond for a selective encapsulation efficiency and controlled release for inhibition of collagen fibrillation

2022 ◽  
Author(s):  
Rasheeda K ◽  
Inbasekar Chandrasekar ◽  
Nishad Fathima Nishter
Keyword(s):  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Acute Disease ◽  
Fibrotic Disorders

Recently, researchers are involved in finding a cure for fibrotic disorders, which is an acute disease. Along with an ideal drug, a superlative carrier is required for developing a sustainable...

scholarly journals Preparation and Sustained-Release Performance of PLGA Microcapsule Carrier System

Nanomaterials ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1758
Author(s):  
Shuaikai Ren ◽  
Chunxin Wang ◽  
Liang Guo ◽  
Congcong Xu ◽  
Yan Wang ◽  
...  
Keyword(s):  
Controlled Release ◽  
Biomedical Applications ◽  
Encapsulation Efficiency ◽  
Drug Carriers ◽  
Optimum Conditions ◽  
Carrier System ◽  
Preparation Conditions ◽  
Encapsulation Rate ◽  
Release Drug ◽  
Release Curve

Microcapsules have been widely studied owing to their biocompatibility and potential for application in various areas, particularly drug delivery. However, the size of microcapsules is difficult to control, and the size distribution is very broad via various encapsulation techniques. Therefore, it is necessary to obtain microcapsules with uniform and tailored size for the construction of controlled-release drug carriers. In this study, emulsification and solvent evaporation methods were used to prepare a variety of ovalbumin-loaded poly (lactic-co-glycolic acid) (PLGA) microcapsules to determine the optimal preparation conditions. The particle size of the PLGA microcapsules prepared using the optimum conditions was approximately 200 nm, which showed good dispersibility with an ovalbumin encapsulation rate of more than 60%. In addition, porous microcapsules with different pore sizes were prepared by adding a varying amount of porogen bovine serum albumin (BSA) to the internal water phase. The release curve showed that the rate of protein release from the microcapsules could be controlled by adjusting the pore size. These findings demonstrated that we could tailor the morphology and structure of microcapsules by regulating the preparation conditions, thus controlling the encapsulation efficiency and the release performance of the microcapsule carrier system. We envision that this controlled-release novel microcapsule carrier system shows great potential for biomedical applications.

scholarly journals Development and properties of a new doxorubicin carrier based on surface-modified iron zero-valent microparticles with high encapsulation efficiency and the possibility of its controlled release

2019 ◽  
Vol 18 (2) ◽  
pp. 69-79
Author(s):  
A. Di Martino ◽  
S. S. Vlasov ◽  
A. M. Guryev ◽  
M. S. Yusubov ◽  
P. S. Postnikov ◽  
...  
Keyword(s):  
Surface Modification ◽  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Chemotherapeutic Agent ◽  
Ultrasound Irradiation ◽  
Zero Valent Iron ◽  
Loading Capacity ◽  
Ph Values ◽  
Release Studies ◽  
Surface Modified

Currently, chemotherapy combined with surgery and radiation therapy is the most effective treatment for cancer. At the same time, the use of this method is accompanied by serious side effects caused by the lack of specificity of most chemotherapeutic agents. In this regard, the development of drug delivery systems (DDS) capable of addressing a chemotherapeutic agent to cancer cells, as well as its controlled release, is a promising approach for the effective treatment of cancer. The aim of the study is to synthesize a new DDS based on surface-modified microparticles of zero-valent iron, to study its properties as a carrier of a chemotherapeutic agent (encapsulation efficiency, loading capacity, possibility of controlled release of a chemotherapeutic agent) and safety. Materials and methods. The microparticles were synthesised by reduction of iron (III) chloride with sodium borohydride followed by in situ surface modification by 4-carboxybenzyldiazonium tosylate. To confirm the occurrence of the reaction, FTIR spectroscopy (Nicolet iS5 Infrared Spectrometer (Thermo Scientific, USA)) was used. Hydrodynamic diameter and surface charge of the microparticles in solution were investigated by dynamic light scattering (DLS) and z-potential. DOX release studies were performed in simulated physiological conditions (pH 3.3; 5.5; 7.4) to evaluate the effect of the external pH on the release rate. Release studies under ultrasound irradiation were performed simultaneously in the same conditions. The effect of surface modification on encapsulation efficiency was evaluated at various pH values (3.3; 5.5; 7.4) and doxorubicin concentrations (0.2; 0.35; 0.5; 0.75; 1.0 mg/ml). To demonstrate the safety of the developed system, cytotoxicity studies were performed on HeLa cell lines (ATCC® CCL-2™). Results. An original method of preparation of the drug carrier, based on iron zero-valent microparticleswith covalently attached chitosan (Fe-CS) on their surface was proposed. Prepared microparticles demonstrated high encapsulation efficiency, drug loading capacity of DOX (0.9 mg per 1 mg of FeCS microparticles), low cytotoxicity and also a possibility to modulate the release rate by ultrasound irradiation and by changing pH of the external environment. Conclusion. A carrier based on microparticles of zero-valent iron with covalently attached to the surface chitosan (Fe-CS) was obtained. The efficiency of encapsulation, the loading capacity of doxorubicin was determined and the possibility of its controlled release under the influence of an ultrasonic field at different pH values was confirmed. In an in vitro experiment on the HeLa cell line (ATCC® CCL-2™), no toxicity was established for all samples (Fe0, Fe-COOH и Fe-CS), regardless of their concentration.

scholarly journals DRUMSTICK MUCILAGE MICROSPHERES FOR CONTROLLED RELEASE OF LAMIVUDINE: DESIGN, OPTIMIZATION AND IN VITRO EVALUATION

2019 ◽  
pp. 60-68
Author(s):  
Santosh G Gada ◽  
ANANDKUMAR Y. ◽  
C. MALLIKARJUN SETTY
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Drug Encapsulation ◽  
Two Factors ◽  
Desirability Approach ◽  
Predicted Values ◽  
Drug Encapsulation Efficiency

Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage. Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design. Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism. Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.

scholarly journals Formulation of Lipoprotein Microencapsulated Beadlets by Ionic Complexes in Algae-Based Carbohydrates

Coatings ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 302
Author(s):  
Alexandru Vasile Rusu ◽  
Florin Leontin Criste ◽  
Daniel Mierliţă ◽  
Claudia Terezia Socol ◽  
Monica Trif
Keyword(s):  
Biological Activity ◽  
Controlled Release ◽  
Sodium Alginate ◽  
Calcium Ions ◽  
Encapsulation Efficiency ◽  
Ionic Complexes ◽  
Inert Environment ◽  
Hpmc Capsules ◽  
Kappa Carrageenan ◽  
Β Carotene

The present study aims to produce sustained-release algae-based carbohydrate microbeadlets of lipoproteins rich-in carotenoids extracted from organic sea buckthorn fruits. β-carotene represented the major compound of the lipoproteins extracts. Emulsification and algae-based carbohydrates, such as sodium-alginate and kappa-carrageenan, provide an inert environment, allowing the embedded targeted bioactive compounds—lipoproteins rich in carotenoids in our case—to maintain greater biological activity and to have a better shelf life. Furthermore, the microbeadlets prepared from sodium-alginate–kappa-carrageenan (0.75%:0.75% w/v) crosslinked with calcium ions showing 90% encapsulation efficiency have been utilized in HPMC capsules using beadlets-in-a-capsule technology, to use as a delivery system for the finished product. The GI simulated tests performed under laboratory conditions suggested that the sodium-alginate–kappa–carrageenan combination could be useful for the formulation-controlled release of microbeadlets containing lipoproteins rich in carotenoids.

Alginate–Chitosan Nanocapsules for Controlled Release of Low Molecular Drugs Tegafur and DHAD

2013 ◽  
Vol 647 ◽  
pp. 264-268 ◽  
Author(s):  
Yuan Gang Liu ◽  
Hong Hao Mao ◽  
Shi Bin Wang ◽  
Qing Qing Sun
Keyword(s):  
Controlled Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Burst Release ◽  
Two Stage ◽  
Cumulative Release ◽  
Stage Process

Alginate–chitosan nanocapsules (Alg-CS NCs) were prepared by a two-stage process. The NCs were loaded with two low molecular drugs-tegafur and Mitoxantrone Hydrochloride(DHAD). Results revealed that these two drugs exhibited different drug loading and release characteristics. The drug loading and encapsulation efficiency of tegafur (<1%) were both lower than those of DHAD with the drug loading at about 20%~60% and encapsulation efficiency over 90%. However, tegafur showed a visible burst release phenomenon and the cumulative release rate of tegafur was much higher than that of DHAD.

scholarly journals Fabrication of Bio-Nanocomposite Based on HNT-Methionine for Controlled Release of Phenytoin

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2576
Author(s):  
Majid Abdouss ◽  
Nastaran Radgoudarzi ◽  
Alireza Mohebali ◽  
Elaheh Kowsari ◽  
Mojtaba Koosha ◽  
...  
Keyword(s):  
Controlled Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Release Profile ◽  
Burst Release ◽  
Loading Efficiency ◽  
Phenytoin Sodium ◽  
Good Potential ◽  
Ft Ir

In this study, a novel promising approach for the fabrication of Halloysite nanotube (HNT) nanocomposites, based on the amino acid named Methionine (Met), was investigated. For this purpose, Met layered on the outer silane functionalized surface of HNT for controlled release of Phenytoin sodium (PHT). The resulting nanocomposite (MNT-g-Met) was characterized by FTIR, XRD, Zeta potential, TGA, TEM and FE-SEM. The FT-IR results showed APTES and Met peaks, which proved the modification of the HNTs. The zeta-potential results showed the interaction between APTES (+53.30) and Met (+38.80) on the HNTs (−30.92). The FE-SEM micrographs have displayed the grafting of Met on the modified HNTs due to the nanotube conversion to a rough and indistinguishable form. The amount of encapsulation efficiency (EE) and loading efficiency (LE) of MNT-g-Met was 74.48% and 37.24%, while pure HNT was 57.5%, and 28.75%, respectively. In-vitro studies showed that HNT had a burst release (70% in 6 h) in phosphate buffer while MNT-g-Met has more controlled release profile (30.05 in 6 h) and it was found to be fitted with the Korsmeyer-Peppas model. Due to the loading efficiency and controlled release profile, the nanocomposite promote a good potential for drug delivery of PHT.

scholarly journals Iron Encapsulation by Deacetylated Glucomannan as an Excipient Using the Gelation Method: Characteristics and Controlled Release

2021 ◽  
Vol 60 (1) ◽  
Author(s):  
Dyah H. Wardhani ◽  
Fatiha N. Etnanta ◽  
Hana N. Ulya ◽  
Nita Aryanti
Keyword(s):  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Experimental Approach ◽  
Weibull Model ◽  
Iron Release ◽  
Scientific Contribution ◽  
Deacetylation Degree ◽  
The Matrix ◽  
Encapsulation Process ◽  
Cacl2 Solution

Research background. Deacetylation and the use of CaCl2 as a gelation agent improve the performance of glucomannan as iron encapsulant using the gelation method. This study was conducted to investigate the effects of deacetylation using NaOH and pH gelation on the characteristics of encapsulated iron using the CaCl2 gelation method. Experimental approach. Glucomannan was deacetylated at various NaOH concentrations and was subsequently utilized as an iron excipient using the pipette-dropped gelation method in CaCl2 solution to directly investigate the gelation process of encapsulation. The pH of the gelation solution was also changed. The beads were subsequently vacuum-dried. Results and conclusions. Deacetylation led to lower endothermic peak temperature of the glucomannan than that of the native one. The deacetylation degree (DD) and gelation pH did not significantly affect the diameter of the beads but influenced their appearance and physical characteristics. The backbone of glucomannan was not changed by either the deacetylation degree or the pH of the gelation treatment. The highest encapsulation efficiency (73.27 %) was observed in the encapsulated iron using the glucomannan matrix of the highest deacetylation degree (82.56 %) and gelated in pH=10 solution. The highest deacetylation degree of glucomannan caused the beads to have the highest swelling, which led to the release of a higher amount of iron. Glucomannan deacetylation improved the pH sensitivity of iron encapsulation, in which more iron was released at a pH=6.8 than of pH=1.2. The Weibull model was the best-fitted model to represent the profile of iron release from the deacetylated glucomannan matrix using the gelation method (R2 > 0.93) at pH=6.8 and pH=1.2 solutions. Novelty and scientific contribution. This result supports the application of deacetylated glucomannan using NaOH as a pH-sensitive matrix on iron encapsulation using CaCl2 solution as gelation agent. A higher deacetylation degree leads to the release of a higher amount of iron from the matrix. The encapsulation is not only protecting the iron but also delivering it to the absorption site and controlling the iron release which are useful in supplement formulation. or food fortifications. The results show that the deacetylated glucomannan as the matrix holds more iron in encapsulation process.

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