Synthesys and Characterization of PLA-CNC Matrix for Antidiabetic Drug Release Applications

2020 ◽  
Vol 988 ◽  
pp. 169-174
Author(s):  
Nufus Kanani ◽  
Yenny Meliana ◽  
Endarto Yudo Wardhono ◽  
Rahmayetty ◽  
Sri Agustina ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Loading ◽  
Study Drug ◽  
The Body ◽  
Raw Material ◽  
Poly Lactic Acid ◽  
Burst Release ◽  
Antidiabetic Drug

Recently, drug nanoparticles formulation using Poly Lactic Acid-Cellulose nanocrystal (PLA-CNC) have been introduced. PLA-CNC were prepared by emulsion method for antidiabetic drug delivery applications. PLA is one of polymer which potentially used as raw material of drug delivery because it has the ability to bind and carry drugs into cell target, but the hydrophilic character of PLA can cause the degradation of PLA in the body run slowly, so it is necessary combining PLA with CNC to improve its property. In this study, special attention has been given to the modification of PLA-CNC as a drug delivery matrix to obtain the optimum drug release of antidiabetic drugs. In this study drug release analysis was conducted at 35-39 °C and pH range 3 to 9 with varied of time dissolution 0 to 180 min. PLA-CNC matrixs were characterized using FTIR and SEM, its drug loading capacity, encapsulation efficiency and in vitro drug release behavior was determined by using UV spectrophotometer. It gave the initial burst release at the first hour at 37 °C pH 3.

NANOMEDICINES: DELIVERING DRUGS USING BOTTOM UP NANOTECHNOLOGY

2005 ◽  
Vol 04 (05n06) ◽  
pp. 855-861 ◽  
Author(s):  
MARTIN GARNETT
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Biodegradable Polymers ◽  
Drug Loading ◽  
Dna Delivery ◽  
Delivery Systems ◽  
The Body ◽  
Nanosized Materials

The use of nanosized materials changes the way in which drugs are handled by the body and offers opportunities to improve drug delivery. The physiological mechanisms controlling the distribution of nanosized materials (enhanced permeability and retention effect, cellular uptake pathways and opsonisation/elimination of nanoparticles) are described. Two different nanosized drug delivery systems are considered; drug delivery and DNA delivery. The deficiencies of currently available biodegradable polymers for preparation of drug containing nanoparticles are mainly the amount of drug that can be incorporated and the rapid rate of drug release. The development of new biodegradable polymers which can interact with the drug and so significantly increase drug loading and decrease the rate of drug release are outlined. DNA delivery necessitates overcoming a variety of biological barriers. We are developing polyelectrolyte complexes of DNA with cationic polyamidoamines (PAA) as a delivery system. Complexing PAA with DNA results in good transfection of cells in vitro. However, in vivo, a more complex arrangement of PAA, Polyethylene glycol-PAA copolymers, DNA and the use of ligands will be required. Despite these efforts, further developments will be needed in nanotechnology for both drug and DNA nanoparticle delivery systems to achieve our clinical objectives.

scholarly journals Formulation and In-Vitro Evaluation of Niosomal drug Delivery in Cancer Chemotherapy

2017 ◽  
Vol 5 (04) ◽  
pp. 29-33
Author(s):  
Naresh Kalra ◽  
G. Jeyabalan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
The Body ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Ethanol Injection

Drug delivery systems are defined as formulations aim for transportation of a drug to the desired area of action within the body. The aim of the study was to investigate the feasibility of using Niosomes as a drug delivery system for Cisplatin By entrapment of drug in Niosomes, dose also could be reduced. Niosomes were prepared by Ethanol injection method using cholesterol and Surfactant. Particle size, zeta potential, entrapment efficiency and in vitro drug release studies were performed. The targeted niosome delivery system is composed of drug, surfactant and cholesterol. With regard to the influence of formulation variables on the percent drug loading (PDL), different compositions with varying ratios of surfactant and cholesterol were studied. In –Vitro drug release mechanism was studied for 24 hours.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

scholarly journals Thermosensitive Chitosan Hydrogels Containing Polymeric Microspheres for Vaginal Drug Delivery

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
Author(s):  
Ting-Ting Yang ◽  
Yuan-Zheng Cheng ◽  
Meng Qin ◽  
Yong-Hong Wang ◽  
Hong-Li Yu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Delivery System ◽  
Drug Loading ◽  
Great Promise ◽  
Burst Release ◽  
Bletilla Striata ◽  
Vaginal Drug Delivery ◽  
Thermosensitive Hydrogels

Thermosensitive hydrogels have increasingly received considerable attention for local drug delivery based on many advantages. However, burst release of drugs is becoming a critical challenge when the hydrogels are employed. Microspheres- (MS-) loaded thermosensitive hydrogels were thus fabricated to address this limitation. Employing an orthogonal design, the spray-dried operations of tenofovir (TFV)/Bletilla striata polysaccharide (BSP)/chitosan (CTS) MS were optimized according to the drug loading (DL). The physicochemical properties of the optimal MS (MS F) were characterized. Depending on the gelation temperature and gelating time, the optimal CTS-sodium alginate- (SA-) α,β-glycerophosphate (GP) (CTS-SA-GP) hydrogel was obtained. Observed by scanning electron microscope (SEM), TFV/BSP/CTS MS were successfully encapsulated in CTS-SA-GP. In vitro releasing demonstrated that MS F-CTS-SA-GP retained desirable in vitro sustained-release characteristics as a vaginal delivery system. Bioadhesion measurement showed that MS-CTS-SA-GP exhibited the highest mucoadhesive strength. Collectively, MS-CTS-SA-GP holds great promise for topical applications as a sustained-release vaginal drug delivery system.

scholarly journals Preparation and characterization of azathioprine microspheres for colon specific delivery

2019 ◽  
Vol 9 (2) ◽  
pp. 97-101
Author(s):  
Rinku Gonekar ◽  
Mohan Lal Kori
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Study Drug ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Intestinal Fluid ◽  
Drug Release Profile ◽  
Fecal Matter

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine.  Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size,  drug entrapment efficiency, percentage yield, shape and surface morphology  and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months. Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.

scholarly journals Influence of sterilization on the drug release behaviour of drug coated silicone

2021 ◽  
Vol 7 (2) ◽  
pp. 672-675
Author(s):  
Katharina Wulf ◽  
Stefan Raggl ◽  
Thomas Eickner ◽  
Gerrit Paasche ◽  
Niels Grabow
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Polymer Coating ◽  
Drug Loading ◽  
In Vitro Release ◽  
Physical Chemical ◽  
Release Studies ◽  
Vitro Release ◽  
Dual Drug

Abstract Sterilization processes ensure sterility of drug delivery systems, but may negatively affect the properties of biomaterials and incorporated drugs by changing their physical, chemical, mechanical properties and drug release behaviour. Therefore, it is important to investigate their influence. In this study, the influence of ethylene oxide (EtO) sterilization on the drug loading and release behaviour of incorporated Diclofenac (DCF) in a Poly-L-lactide (PLLA) coating and Dexamethasone (DMS) in the silicone carrier is presented. Silicone samples containing DMS were coated with PLLA containing DCF varying in layer thickness (5, 10, and 20 μm). Half of the samples underwent EtO sterilization, the other half was not sterilized. All un-/sterilized sample surfaces were in view of the morphology and hydrophilicity examined. Furthermore, in vitro release studies of DMS and DCF were conducted. The sterilized sample surfaces showed no morphological and hydrophilicity changes. The DCF and DMS loadings were similar for the sterile and untreated samples. This also applied to the in vitro DMS release profiles apart from the end of the studies where slight differences were evident. The results indicate that both drugs loaded in the polymer coating and the silicone were not impaired by the sterilization process. Thus, EtO sterilization appears suitable for DMS containing silicone and DCF incorporated PLLA coatings as a dual drug delivery system.

scholarly journals Zirconium-Porphyrin PCN-222: pH-responsive Controlled Anticancer Drug Oridonin

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Xin Leng ◽  
Hongliang Huang ◽  
Wenping Wang ◽  
Na Sai ◽  
Longtai You ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hepg2 Cells ◽  
Drug Loading ◽  
Annexin V ◽  
Controlled Drug Release ◽  
Dapi Staining ◽  
High Drug ◽  
High Drug Loading

Drug delivery carriers with a high drug loading capacity and biocompatibility, especially for controlled drug release, are urgently needed due to the side effects and frequent dose in the traditional therapeutic method. Guided by nanomaterials, we have successfully synthesized zirconium-based metal−organic frameworks, Zr-TCPP (TCPP: tetrakis (4-carboxyphenyl) porphyrin), namely, PCN-222, which is synthesized by solvothermal method. And it has been designed as a drug delivery system (DDS) with a high drug loading of 38.77 wt%. In our work, PCN-222 has achieved pH-sensitive drug release and showed comprehensive SEM, TEM, PXRD, DSC, FTIR, and N2 adsorption-desorption. The low cytotoxicity and good biocompatibility of PCN-222 were certificated by the in vitro results from an MTT assay, DAPI staining, and Annexin V/PI double-staining even cultivated L02 cells and HepG2 cells for 48h. Furthermore, Oridonin, a commonly used cancer chemotherapy drug, is adsorbed into PCN-222 via the solvent diffusion technique. Based on an analysis of the Oridonin release profile, results suggest that it can last for more than 7 days in vitro. And cumulative release rate of Ori at the 7 d was about 86.29% and 63.23% in PBS (pH 5.5 and pH 7.2, respectively) at 37°C. HepG2 cells were chosen to research the cytotoxicity of PCN-222@Ori and free Oridonin. The results demonstrated that the PCN-222@Ori nanocarrier shows higher cytotoxicity in HepG2 cells compared to Oridonin.

Combine Drug Delivery of Thymoquinone-Doxorubicin by Cockle Shellderived pH-sensitive Aragonite CaCO3 Nanoparticles

2020 ◽  
Vol 10 (4) ◽  
pp. 518-533 ◽  
Author(s):  
Kehinde M. Ibiyeye ◽  
Abu B.Z. Zuki ◽  
Norshariza Nurdin ◽  
Mokrish Ajat
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Calcium Carbonate ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Multiple Drug ◽  
Burst Release ◽  
Cockle Shell

Background: Cockleshell-derived aragonite calcium carbonate nanoparticles were prepared by the top-down approach for combine delivery of two types of drugs. Objective: The aim of this study was to synthesize and characterize thymoquinone-doxorubicin loaded cockle shell-derived aragonite calcium carbonate nanoparticle. Aragonite calcium carbonate nanoparticles encapsulating thymoquinone and doxorubicin alone were also prepared. Methods: The blank and drug-loaded nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Zeta potential, Fourier transformed infrared and X-ray diffraction. Drug delivery properties, in vitro drug release study at pH 7.4, 6 and 4.8, and effect of blank nanoparticles on MCF10A, 3T3, MDA MB231 cells were also analyzed. Results: The blank and drug-loaded nanoparticles were pleomorphic and their sizes varying from 53.65 ± 10.29 nm to 60.49 ± 11.36 nm with an overall negative charge. The entrapment efficiency of thymoquinone and doxorubicin were 41.6 and 95.8, respectively. The FTIR showed little alteration after loading thymoquinone and doxorubicin while XRD patterns revealed no changes in the crystallizations of nanoparticles after drug loading. The drug release kinetics of doxorubicin and thymoquinone from the nanoparticles showed a continuous and gradual release after an initial burst release was observed. At pH 4.8, about 100% of drug release was noticed, 70% at pH 6 while only 50% at pH 7.4. The cell viability was 80% at a concentration of 1000 ug/ml of blank nanoparticle. Conclusion: The cockle shell-derived pH sensitive aragonite calcium carbonate nanoparticle provides an effective and simple means of multiple drug delivery and function as a platform for pH controlled release of loaded therapeutic agents.

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