Sinefungin-PLGA Nanoparticles: Drug Loading, Characterization, In Vitro Drug Release and In Vivo Studies

2009 ◽  
Vol 9 (1) ◽  
pp. 150-158 ◽  
Author(s):  
Sendilcoumare Kalimouttou ◽  
Mohamed Skiba ◽  
Pierre Bon ◽  
Pierre Déchelotte ◽  
Philippe Arnaud ◽  
...  
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Plga Nanoparticles

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

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 Effect of A 2-HP-β-Cyclodextrin Formulation on the Biological Transport and Delivery of Chemotherapeutic PLGA Nanoparticles

2020 ◽  
Author(s):  
Kangyu Zheng ◽  
Zeju Huang ◽  
Jiaying Huang ◽  
Xiangmei Liu ◽  
JUNFENG BAN ◽  
...  
Keyword(s):  
Drug Release ◽  
Cellular Uptake ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Human Lung Cancer ◽  
Pharmacokinetic Analysis ◽  
Biological Transport ◽  
Sustained Drug Release

Abstract Background: The aim of this work was to develop a novel and feasible modification strategy by utilizing the supramolecular effect of 2-hydroxypropyl-beta-cyclodexrin (2-HP-β-CD) for enhancing the biological transport efficiency of paclitaxel (PTX)-loaded poly(lactide-co-glycolide)(PLGA) nanoparticles.Methods: PTX-loaded 2-HP-β-CD-modified PLGA nanoparticles (2-HP-β-CD/PLGA NPs) were prepared using the modified emulsion method. Nano-characteristics, drug release behavior, in vitro cytotoxicity, cellular uptake profiles and in vivo bio-behavior of the nanoparticles were then characterized. Results: Compared with the plain PLGA NPs, 2-HP-β-CD/PLGA NPs exhibited smaller particle sizes (151.03±1.36 nm), increased entrapment efficiency (~49.12% increase) and sustained drug release. When added to A549 human lung cancer cells, compared with PLGA NPs, 2-HP-β-CD/PLGA NPs exhibited higher cytotoxicity in MTT assays and improved cellular uptake efficiency. Pharmacokinetic analysis showed that the AUC value of 2-HP-β-CD/PLGA NPs was 2.4-fold higher than commercial Taxol® and 1.7-fold higher than plain PLGA NPs. In biodistribution assays, 2-HP-β-CD/PLGA NPs exhibited excellent stability in the circulation.Conclusions: The results of this study suggest that formulation contains 2-HP-β-CD can prolong PTX release, enhance drug transpot efficiency and serve as a potential tumor targeting system for PTX.

Pharmacokinetic Profile of Oxaliplatin-Loaded pH-Responsive Hydrogels in Rabbits

2020 ◽  
Vol 26 (44) ◽  
pp. 5755-5763
Author(s):  
Kaleem Ullah ◽  
Shujaat Ali Khan ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Ghulam Murtaza
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Oral Solution ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Platinum Compound ◽  
In Vivo Evaluation ◽  
Significant Difference

Background: Oxaliplatin (OXP), a 3rd generation platinum compound, which causes severe side effects due to; impulse high concentration in the bloodstream thereby exposing healthy cells at a high ratio, nonspecific delivery at the target site and non-compliance is administered intravenously. Objective: The project was aimed at the development, characterization, and in-vitro and in-vivo evaluation of pHresponsive hydrogels for oral administration of OXP. Methods: Hydrogel formulations were synthesized through a free radical polymerization technique followed by brief characterization using various techniques. The hydrogels were investigated for various in-vitro studies such as sol-gel, drug loading, swelling, drug release, and MTT-assay. While in-vivo studies such as oral tolerability, histopathology, and hematology studies were performed on rabbits. A simple and sensitive HPLC-UV method was optimized and the comparative pharmacokinetic study was performed in rabbits using OXP-oral solution and OXP-loaded hydrogels. Results: In-vitro characterization confirmed that the reactant was successfully crosslinked to form thermally stable hydrogels with decreased crystallinity and rough surface. Swelling and drug release showed that hydrogels were more responsive to basic pH (6.8 and 7.4) in comparison with pH 1.2. The blank hydrogels were cytocompatible as more than 95% of the cells were viable while free OXP and OXP-loaded hydrogels displayed dosedependent cytotoxic effect. In-vivo studies confirmed that chitosan and gelatin hydrogel suspension was well tolerable up to 3800 mg/kg and 4000 mg/kg of body weight, respectively. Hematology and serum chemistry reports were well within the range suggesting normal liver and kidney functions. Similarly, histopathology slides of rabbit vital organs were also found normal without causing any histopathological change. Conclusion: HPLC-UV method was successfully optimized for OXP detection in oral solution and hydrogels administered to rabbits. A significant difference was found among various pharmacokinetic parameters by comparing the two groups including half-life (t1/2), tmax, Cmax, AUCtot MRT, Vz, and Lz.

scholarly journals Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

2013 ◽  
Vol 63 (3) ◽  
pp. 359-372 ◽  
Author(s):  
Naresh Vishal Gupta ◽  
Shirodker Natasha ◽  
Anil Getyala ◽  
Ramnath Sudeendra Bhat
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Drug Loading ◽  
Particle Size Analysis ◽  
Vaginal Candidiasis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Dsc Studies

Abstract The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

scholarly journals State-of-the-Art Irradiation Technology for Polymeric Hydrogel Fabrication and Application in Drug Release System

2021 ◽  
Vol 8 ◽  
Author(s):  
Muhammad Asim Raza ◽  
Jin-Oh Jeong ◽  
Sang Hyun Park
Keyword(s):  
Drug Release ◽  
Gamma Ray ◽  
Drug Loading ◽  
High Energy ◽  
Single Step ◽  
Antibiotic Drugs ◽  
Gamma Ray Irradiation ◽  
Polymeric Hydrogels

Chronic and debilitating diseases can be marginally cured by anti-inflammatory, antiseptic, and antibiotic drugs, there is still need for more efficacious delivery approaches. Biodegradable and biocompatible polymeric hydrogels are essential requirements for drug release systems due to sustained or targeted drug delivery. Irradiation crosslinking of polymers is considered a safe route for the fabrication of hydrogels because crosslinking takes place without addition of unnecessary toxic reagents such as initiators or crosslinkers. This technology is a useful way to induce sterilization and crosslinking in a single step. Several natural and synthetic polymers in different combinations are crosslinked through high energy ionizing radiation such as electron beam and gamma ray irradiation. Polymeric hydrogels prepared using these techniques exhibit good gel fraction, swelling ratio, and mechanical properties. In addition, hydrogels possess drug loading and release characteristics, antimicrobial characteristics, and in-vivo/in-vitro cytocompatibility. The advantage of biodegradable and biocompatible drug release systems is the controlled release of drugs without deleterious effects on targeted sites. This mini review about irradiation crosslinked hydrogels will provide sufficient guidelines for new researchers to proceed further in this field.

scholarly journals Preparation and Release Profiles in Vitro/Vivo of Galantamine Pamoate Loaded Poly (Lactideco-Glycolide) (PLGA) Microspheres

2021 ◽  
Vol 11 ◽  
Author(s):  
Liping Du ◽  
Shankui Liu ◽  
Guizhou Hao ◽  
Li Zhang ◽  
Miaomiao Zhou ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Solvent Evaporation Method ◽  
Sustained Drug Release ◽  
Water Emulsion ◽  
Oil Water

Patient’s poor compliance and the high risk of toxic effects limit the clinical use of galantamine hydrobromide. To overcome these drawbacks, the sustained-release galantamine pamoate microspheres (GLT-PM-MS) were successfully developed using an oil/water emulsion solvent evaporation method in this study. Physicochemical properties of GLT-PM-MS were carefully characterized, and the in vitro and in vivo drug release behaviors were well studied. Results showed that the morphology of optimized microspheres were spherical with smooth surfaces and core-shell interior structure. Mean particle size, drug loading and entrapment efficiency were 75.23 ± 1.79 μm, 28.01 ± 0.81% and 87.12 ± 2.71%, respectively. The developed GLT-PM-MS were found to have a sustained release for about 24 days in vitro and the plasma drug concentration remained stable for 17 days in rats. These results indicated that GLT-PM-MS could achieve the sustained drug release purpose and be used in clinical trial.

FORMULATION AND EVALUATION OF MICROSPHERES FOR NASAL DELIVERY OF ANTI-HYPERTENSIVE DRUG

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (10) ◽  
pp. 21-26
Author(s):  
S. S Shelake ◽  
◽  
R. M Mhetre ◽  
S. V Patil ◽  
S. S Patil ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Nasal Delivery ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Hypertensive Drug

Lisinopril is used in the treatment of hypertension and heart failure in myocardial infarction and also in diabetic nephropathy. It is very poorly absorbed from GIT. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers may provide a significant increase in the nasal residence time. The microspheres prepared by emulsion solvent evaporation method were characterized for encapsulation efficiency, drug loading, particle size, surface morphology, degree of swelling, ex vivo mucoadhesion, drug release and ex vivo diffusion studies. Entrapment efficiency of microspheres was in range of 84.95±0.50% to 97.44±0.61% mucoadhesion was 83.76% and 94.41% and drug release up to 40 minutes was 53.66% to 88.32%. In ex vivo studies, the microspheres showed good bioavailability by nasal route compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres are better than single carbopol-based formulation for the delivery of lisinopril.

Different pH-Values of Release Medium Influence the Drug Release from PTX-PCL Microspheres

2012 ◽  
Vol 482-484 ◽  
pp. 2605-2608 ◽  
Author(s):  
Li Li Ruan ◽  
Da Xin Wang ◽  
You Wei Zhang ◽  
Jiong Xin Zhao ◽  
Xiu Fang Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
High Performance ◽  
Drug Loading ◽  
In Vitro Release ◽  
Buffer Solution ◽  
Ph Values ◽  
Sustained Release Microspheres

In this paper we study in vitro release of paclitaxel-loade polycaprolactone sustained-release microspheres. Different pH values release medium is used to simulate pH conditions in different parts of body, and determination the paclitaxel in Microspheres by High Performance Liquid Chromatography according Chinese Pharmacopoeia 2010. The experimental results indicate that the microspheres release rates of same drug loading content in buffer solution of pH 7.35 is the fastest, and in the pH 1.2 is the slowest. The drug release behavior according to the first-order model and it is not affected by drug loading rate of microspheres. The prepared paclitaxel-loade polycaprolactone sustained-release microspheres has good sustained release effect in different release media, and the results can provide references for further study of in vivo release.

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