scholarly journals Anti-tumor Effect of Quercetin Loaded Chitosan Nanoparticles on Induced Colon Cancer in Wistar Rats

2019 ◽  
Vol 9 (3) ◽  
pp. 409-415 ◽  
Author(s):  
Jalil Rashedi ◽  
Amir Ghorbani Haghjo ◽  
Mehran Mesgari Abbasi ◽  
Ali Dastranj Tabrizi ◽  
Shadi Yaqoubi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Treatment Group ◽  
Drug Release ◽  
Wistar Rats ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Physicochemical Characterization ◽  
Microvascular Density ◽  
Site Specific

Purpose: This study was aimed to evaluate the site-specific drug delivery of 5-FU with chitosan (CS) as a carrier and quercetin (Qu) against induced colon cancer in Wistar rats. Methods: Cross-linked CS-Qu nanoparticles (NPs) were prepared by ionotropic gelation method. Physicochemical characterization of NPs was performed by Fourier-transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), in vitro drug release, and drug loading efficiency (LE). 1, 2-Dimethylhydrazine (DMH) and dextran sulfate sodium (DSS) were applied to induce adenocarcinoma tumors on inbred male Wistar rats’ colon. The treatment group of rats was administered through enema with NPs dispersion. Hematoxylin and eosin staining were performed to the histopathological examination of tumors. Results: Zeta potential and particle size for NPs were +53.5 ± 5 mV and 179 ± 28 nm, respectively. About 96% Qu LE was obtained with a maximum release of 5.63 ±1.59% and 4.62 ± 1.33% after 24 hours in PB solution with pH values of 6 and 7.4, respectively. The numbers of 8 to 21 tumors were observed in all rats administered with DMH and DSS. Significantly decreasing of microvascular density and mitosis count was detected in the treatment group in comparison with cancerous group (P = 0.032 for the former compared to P = 0.016 for the later), respectively. Furthermore, the treatment group showed a high apoptosis rate (P = 0.038). Conclusion: The developed Qu-loaded CS NPs were good candidates for site-specific and sustained drug release in enema treatment. Decreasing of microvascular density and mitosis count, along with increasing the apoptosis percent in the treatment group proved that the NPs could have promising results in site-specific and sustained drug delivery against colorectal cancer.

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

scholarly journals Polymerisation-induced self-assembly (PISA) as a straightforward formulation strategy for stimuli-responsive drug delivery systems and biomaterials: recent advances

2021 ◽  
Vol 9 (1) ◽  
pp. 38-50
Author(s):  
Hien Phan ◽  
Vincenzo Taresco ◽  
Jacques Penelle ◽  
Benoit Couturaud
Keyword(s):  
Drug Delivery ◽  
Block Copolymers ◽  
Drug Release ◽  
Self Assembly ◽  
Drug Delivery Systems ◽  
Amphiphilic Block Copolymers ◽  
Stimuli Responsive ◽  
Site Specific ◽  
On Demand ◽  
Redox Agents

Stimuli-responsive amphiphilic block copolymers obtained by PISA have emerged as promising nanocarriers for enhancing site-specific and on-demand drug release in response to a range of stimuli such as pH, redox agents, light or temperature.

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.

Nano-engineered electro-responsive drug delivery systems

2016 ◽  
Vol 4 (18) ◽  
pp. 3019-3030 ◽  
Author(s):  
Yi Zhao ◽  
Ana C. Tavares ◽  
Marc A. Gauthier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Drug Loading ◽  
Delivery Systems

Nano-engineering is exploited to address the slow drug release and low drug loading of electro-responsive drug delivery systems.

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.

Preparation and Characterization of Biopolymeric Nanoparticles as Drug Delivery Vehicles

2017 ◽  
pp. 225-246
Author(s):  
Sai S. Sagiri ◽  
Suraj K. Nayak ◽  
S. Lakshmi ◽  
Kunal Pal
Keyword(s):  
Drug Delivery ◽  
Salicylic Acid ◽  
Drug Release ◽  
Chitosan Nanoparticles ◽  
Xrd Analysis ◽  
Gelatin Nanoparticles ◽  
Drug Delivery Vehicles ◽  
Model Drug ◽  
Bioactive Agents

In recent years, the use of biopolymeric nanoparticles as vehicles for drug delivery has increased exponentially. In the present study, chitosan and gelatin nanoparticles were prepared by ionic gelation and desolvation methods, respectively. Salicylic acid was used as the model drug. The nanoparticles were characterized using SEM, XRD analysis and FTIR spectrophotometric studies. In vitro drug release experiments were carried out to understand the mechanism of drug release. SEM micrographs showed the formation of spherical nanoparticles. XRD studies indicated a higher crystalline nature of the chitosan nanoparticles as compared to the gelatin nanoparticles. FTIR studies indicated the presence of salicylic acid within the drug- loaded nanoparticles. Drug release studies indicated that the developed nanoparticles may be used as carriers for various bioactive agents.

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE LOADED FLOATING MICROSPHERES

2019 ◽  
pp. 74-82
Author(s):  
SHIKHA KESHARVANI ◽  
PANKAJ KUMAR JAISWAL ◽  
ALOK MUKERJEE ◽  
AMIT KUMAR SINGH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Compatibility Study ◽  
Specific Drug ◽  
Site Specific

Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent. Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics. Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism. Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.

Preparation and anti-cancer activity of transferrin/folic acid double-targeted graphene oxide drug delivery system

2020 ◽  
Vol 35 (1) ◽  
pp. 15-27 ◽  
Author(s):  
Taicheng Lu ◽  
Zhenzhen Nong ◽  
Liying Wei ◽  
Mei Wei ◽  
Guo Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Graphene Oxide ◽  
Folic Acid ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
Target Drug Delivery ◽  
Target Drug ◽  
Target Drug Delivery System

In this study, a transferrin/folic acid double-targeting graphene oxide drug delivery system loaded with doxorubicin was designed. Graphene oxide was prepared by ultrasound improved Hummers method and was modified with Pluronic F68, folic acid, and transferrin to decrease its toxicity and to allow dual-targeting. The results show that the double target drug delivery system (TFGP*DOX) has good and controllable drug delivery performance with no toxicity. Moreover, TFGP*DOX has a better inhibitory effect on SMMC-7721 cells than does a single target drug delivery system (FGP*DOX). The results of drug release analysis and cell inhibition studies showed that TFGP*DOX has a good sustained release function that can reduce the drug release rate in blood circulation over time and improve the local drug concentration in or near a targeted tumor. Therefore, the drug loading system (TFGP*DOX) has potential application value in the treatment of hepatocellular carcinoma.

Multimodal Cancer Treatment: Real Time Monitoring, Optimization, and Synergistic Effects

2008 ◽  
Vol 7 (5) ◽  
pp. 409-414 ◽  
Author(s):  
Gunnar Myhr
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Adjuvant Therapy ◽  
Ionizing Radiation ◽  
Cancer Treatment ◽  
Real Time ◽  
Treatment System ◽  
Multi Drug Resistance ◽  
Real Time Monitoring ◽  
Site Specific

The primary objective of this analysis is to provide the theoretical framework for a novel multimodal cancer treatment system emphasizing the use of ultrasound as a synergistic drug release mechanism, real time monitoring by MRI of hyperthermic, pO2, and ultrasound induced released effects. The aim is to provide a cure for the 20% of cancer victims who will die of complications from local solid tumors. Adjuvant therapy usually refers to surgery preceding or following chemotherapy and/or ionizing radiation treatment to decrease the risk of recurrence, but the absolute benefit for survival obtained with adjuvant therapy compared to control is only approximately 6%. Tumor hypoxia represents a primary therapeutic concern, besides multi-drug resistance (MDR), because it can reduce the effectiveness of drugs and radiotherapy; well-oxygenated cells require one-third the dose of hypoxic cells to achieve a given level of cell killing. The era of systemic and indiscriminate chemotherapeutic drug delivery into both healthy and pathologic tissues is near an end. Targeted drug delivery using nanoparticles is emerging as the new vehicle, either as a single treatment option, as part of adjuvant procedures or as a component of a multimodal cancer treatment system. There are more than 100 nanosized liposomes or particles, and conjugated anticancer agents in various stages of preclinical and clinical development. Active targeting can be achieved by site-specific delivery or site-specific triggering. Ultrasound can be utilized as both a site triggering and synergistic mechanism in drug release. The process can be monitored using MRI by a physical process called cavitation. An analysis of low frequency ultrasound exposure in combination with liposomally encapsulated doxorubicin (Caelyx) on Balb/c nude mice inoculated with a WiDr (human colon cancer) tumor cell line provided tumor growth inhibition of 30–40%. Mild hyperthermia causes mean intratumor pO2 to increase by 25% and enhances tumor radiosensitization. Hyperthermia causes the extravasation of liposome nanoparticles in deep tumor regions. Ionizing radiation improves the distribution and uptake of drugs. Liposomally encapsulated drugs and ultrasound mediated hyperthermia have been proven to circumvent MDR effects. Hyperthermic effects and pO2 monitoring of bodily fluid have been performed by MRI. It is hypothesized that increased vascularization and subsequent increase in pO2 levels to hypoxic regions, and monitoring of drug release through cavitation, can facilitate optimized real time concomitant or sequential treatments of drug therapy, hyperthermia, ionizing radiation, etc., before or after surgery. An improved therapeutic index with the use of the outlined system seems probable.

Sign in / Sign up

Export Citation Format

Share Document