scholarly journals CARMUSTINE LOADED LACTOFERRIN NANOPARTICLES DEMONSTRATES AN ENHANCED ANTIPROLIFERATIVE ACTIVITY AGAINST GLIOBLASTOMA IN VITRO

2018 ◽  
Vol 10 (6) ◽  
pp. 234 ◽  
Author(s):  
Harikiran Athmakur ◽  
Anand Kumar Kondapi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Cellular Uptake ◽  
Stable Distribution ◽  
Drug Loading ◽  
Glioblastoma Cells ◽  
Treatment Regimens ◽  
Microscopic Studies

Objective: Despite sophisticated treatment regimens, there is no significant improvement in the mortality rates of glioblastoma due to insufficient dosage delivery, reoccurrence of tumors, higher systemic toxicity, etc. Since brain endothelial cells and glioblastoma cells express lactoferrin receptors, a target-specific drug delivery vehicle was developed using lactoferrin itself as a matrix, into which carmustine was loaded. The objective was to use carmustine loaded lactoferrin nanoparticles (CLN) to achieve higher therapeutic efficacy and target specificity compared to free carmustine.Methods: CLN were prepared using the Sol-oil method. The nanoparticles prepared were characterized for their size, shape, polydispersity, and stability using FESEM and DLS methods. Drug loading and drug releasing efficiencies were also estimated. Further, cellular uptake of nanoparticles and their antiproliferative efficacy against glioblastoma cells were evaluated.Results: Characterization of CLN showed that they were spherical with ≤ 41 nm diameter and exhibited homogeneously dispersed stable distribution. Loading efficiency of carmustine in CLN was estimated to be 43±3.7 %. Drug release from the nanoparticles was pH dependent with the maximum observed at pH 5. At physiological and gastric pH, drug release was lower, whereas maximum release was observed at endocytotic vesicular and around tumor extracellular pH. Confocal microscopic studies showed an active cellular uptake of nanoparticles. Results of antiproliferative analysis substantiated a higher antiproliferative effect for CLN compared to free carmustine.Conclusion: The results of the study demonstrated that CLN serves as a vital tool, in designing an effective treatment strategy for targeted drug delivery to glioblastoma.

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.

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 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.

scholarly journals Comparison of Polydopamine-Coated Mesoporous Silica Nanorods and Spheres for the Delivery of Hydrophilic and Hydrophobic Anticancer Drugs

2019 ◽  
Vol 20 (14) ◽  
pp. 3408 ◽  
Author(s):  
Anna-Karin Pada ◽  
Diti Desai ◽  
Kaiyao Sun ◽  
Narayana Prakirth Govardhanam ◽  
Kid Törnquist ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Mesoporous Silica ◽  
Cellular Uptake ◽  
Drug Delivery Systems ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Distribution ◽  
Delivery Systems ◽  
Hydrophilic Drugs

Mesoporous silica nanoparticles (MSNs) have been widely studied as drug delivery systems in nanomedicine. Surface coating of MSNs have enabled them to perform efficiently in terms of bioavailability, biocompatibility, therapeutic efficacy and targeting capability. Recent studies have suggested the use of polydopamine (PDA) as a facilitative coating for MSNs that provides sustained and pH-responsive drug release, owing to the adhesive “molecular-glue” function of PDA. This further endows these hybrid MSN@PDA particles with the ability to carry large amounts of hydrophilic drugs. In this study, we expand the feasibility of this platform in terms of exploring its ability to also deliver hydrophobic drugs, as well as investigate the effect of particle shape on intracellular delivery of both a hydrophilic and hydrophobic anticancer drug. MSN@PDA loaded with doxorubicin (hydrophilic) and fingolimod (hydrophobic) was studied via a systematic in vitro approach (cellular internalization, intracellular drug distribution and cytotoxicity). To promote the cellular uptake of the MSN@PDA particles, they were further coated with a polyethylene imine (PEI)-polyethylene glycol (PEG) copolymer. Drug-loaded, copolymer-coated MSN@PDA showed effective cellular uptake, intracellular release and an amplified cytotoxic effect with both doxorubicin and fingolimod. Additionally, rods exhibited delayed intracellular drug release and superior intracellular uptake compared to spheres. Hence, the study provides an example of how the choice and design of drug delivery systems can be tuned by the need for performance, and confirms the PDA coating of MSNs as a useful drug delivery platform beyond hydrophilic drugs.

Preparation and Characterization of Cyclophosphamide-Loaded Chitosan Microspheres

2012 ◽  
Vol 621 ◽  
pp. 130-133
Author(s):  
Yi Lin Ding ◽  
Su Su Ding ◽  
Guo Fang Ding
Keyword(s):  
Drug Release ◽  
Anticancer Agent ◽  
Loading Rate ◽  
Drug Loading ◽  
Average Diameter ◽  
Uv Spectrophotometry ◽  
Chitosan Microspheres ◽  
Dialysis Bag

Chitosan microspheres were prepared by using a cross linking agent combined with an emulsion technique. Cyclophosphamide was loaded as an anticancer agent. Obtained microspheres were spherical and regular, with a smooth surface morphology, having an average diameter of 15.7±9.0μm. After preparation, the drug-loading rate and entrapment rate of cyclophosphamide was investigated by UV spectrophotometry. Drug release was tested in vitro in a dynamic dialysis system with a dialysis bag. The chitosan microspheres prepared were proved to have good drug release profiles.

Macrophage escape by cholesterol-polyoxyethylene sorbitol oleate micelles for pulmonary delivery

Nanomedicine ◽  
2020 ◽  
Vol 15 (5) ◽  
pp. 489-509
Author(s):  
Dong Shen ◽  
Yan Shen ◽  
Qian Chen ◽  
Bin Huang ◽  
Yedong Mi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Ultrasonic Method ◽  
Pulmonary Delivery ◽  
Single Factor ◽  
Box Behnken Design ◽  
Single Factor Experiment

Aim: Micelles are one of the most promising nanoplatforms for drug delivery, and here, cholesterol-conjugated polyoxyethylene sorbitol oleate (CPSO) micelles have been fabricated for the pulmonary delivery of paclitaxel (PTX). Materials & methods: PTX-CPSO micelles were prepared by a dialysis-ultrasonic method, and a single-factor experiment with a Box–Behnken design was conducted to optimize the formulation. Furthermore, intracellular and phagocytosis escape studies of the optimized formulation were performed on A549 and NR8383 cells. Results: The optimal micelles exhibited satisfactory encapsulation efficiency (78.48 ± 2.36%) and drug loading (17.06 ± 1.71%). In vitro studies showed enhanced CPSO micelle A549 cellular uptake and their ability to escape macrophages. Conclusion: PTX-CPSO micelles could be a promising system for pulmonary targeting by intravenous administration.

Redox-sensitive hyaluronic acid–paclitaxel conjugate micelles with high physical drug loading for efficient tumor therapy

2015 ◽  
Vol 6 (46) ◽  
pp. 8047-8059 ◽  
Author(s):  
Tingjie Yin ◽  
Jing Wang ◽  
Lifang Yin ◽  
Linjia Shen ◽  
Jianping Zhou ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Drug Release ◽  
Cellular Uptake ◽  
Drug Loading ◽  
Tumor Therapy ◽  
Drug Conjugates ◽  
Self Assembled ◽  
Polymer Drug Conjugates

Characterization of targeted redox-sensitive micelles self-assembled from polymer–drug conjugates exhibiting conspicuous drug loading capabilities, selective cellular uptake, rapid intracellular disassembly and drug release is presented.

Sign in / Sign up

Export Citation Format

Share Document