Development and Evaluation of Nanoparticle-Loaded Hydrogel of Co-trimoxazole

Author(s):  
Prajeesh Kumar ◽  
Raj K. Narang ◽  
Shivansh Swamy

In this study, development of nanoparticle loaded hydrogel of Cotrimoxazole that could simultaneously deliver trimethoprim and sulfamethoxazole at the site of wound to promote and accelerate wound healing is planned. Chitosan nanoparticles loaded with Co-trimoxazole were prepared by ionic gelation method. Chitosan nanoparticles were optimized and F5 formulation was selected 5:1 Chitosan TPP ratio for this Homogenization speed was kept at 5000 rpm and an average size of 209.8 ± 34.6 was obtained, PDI was found to be 0.26 ± 0.04, the zeta potential of the nanoparticles was found to be + 24.7 ± 3.12 and the entrapment efficiency of 89.7 ± 3.1 % was seen. Hydrogel was prepared and optimized on the basis of Conc. of Carbopol 940 1.2%, viscosity 14.953 ± 0.51, pH 5.9 ± 0.04, Swelling index 250 ± 4.71 and Spreadability 34 ± 3.5. Antimicrobial study and Minimum Inhibitory Concentration (MIC) were performed and it was observed that the MIC of Co-trimoxazole was 2 µg/mL and the hydrogel formulation showed maximum zone of inhibition 3.7 ± 0.3 after 72 hours against plain drug and marketed formulation. The rate of wound contraction was calculated in percentage and at 15th day the control group had 72% ± 3.9%, Marketed formulation group had 36% ± 5.2% and the hydrogel formulation had reduced the wound size to mere 4% ± 1.3% only. Hydrogel loaded with nanoparticles of Co-trimoxazole that possessed optimum rheology and provided sustained drug release was successfully prepared. The developed hydrogel formulation was found to heal the wound 1.5 times faster than the marketed formulation thus providing us with a better alternative to other conventional wound dressings.

2013 ◽  
Vol 662 ◽  
pp. 149-152
Author(s):  
Yan Hao ◽  
Hao Wu ◽  
Wei Li ◽  
Xiao Mei Luo ◽  
Kai Zhao

In this study, the researcher’s interest is focused on establishing a model with La Sota live vaccine immobilized into chitosan, which was prepared using a ionic gelation method. The formulation, preparation procedure, influence factors, physicochemical characteristics were evaluated. The results of study demonstrate that the NDV-CS-NPs have been produced with suitable size, morphous regulation, extremely spherical shape, regular and well-distributed. The NDV-CS-NPs produced by the optimal formulation were average size (371.1nm) and proper zata potential (+2.84 mV). The entrapment efficiency was (74±3.7) %. It can provide a new useful information for the development and evaluation of synthetic vaccines.


2020 ◽  
Vol 12 (22) ◽  
pp. 2019-2034
Author(s):  
Neeta Solanki ◽  
Meenu Mehta ◽  
Dinesh Kumar Chellappan ◽  
Gaurav Gupta ◽  
Nicole G Hansbro ◽  
...  

Aim: In the present study boswellic acids-loaded chitosan nanoparticles were synthesized using ionic gelation technique. The influence of independent variables were studied and optimized on dependent variables using central composite design. Methodology & results: The designed nanoparticles were observed spherical in shape with an average size of 67.5–187.2 nm and have also shown an excellent entrapment efficiency (80.06 ± 0.48). The cytotoxicity assay revealed enhanced cytotoxicity for drug-loaded nanoparticles in contrast to the free drug having an IC50 value of 17.29 and 29.59 μM, respectively. Flow cytometry confirmed that treatment of cells with 40 μg/ml had arrested 22.75 ± 0.3% at SubG0 phase of the cell cycle when compared with untreated A459 cells. The observed results justified the boswellic acids-loaded chitosan nanoparticles were effective due to greater cellular uptake, sustained intercellular drug retention and enhanced antiproliferative effect by inducing apoptosis.


2020 ◽  
Vol 35 (6) ◽  
pp. 538-553
Author(s):  
Karuna Sharma ◽  
Pradip Nirbhavane ◽  
Sanjay Chhibber ◽  
Kusum Harjai

Zingerone loaded chitosan nanoparticles (Z-NPs) were developed to deliver the Zingerone across cell membrane and to further enhance its anti-virulence property. The Z-NPs were characterized with respect to size, percentage entrapment efficiency (% EE), zeta potential and percentage drug release. Further the Z-NPs were evaluated for antioxidant DPPH assay, antibiofilm, anti-virulence activities, and gene expression profiles. The developed Z-NPs showed an average size of 390 nm, zeta potential of +56.6 mV, 67% drug entrapment efficiency, and exhibited pH dependent controlled release of Zingerone over a period of 5 days (up to 80%). The Z-NPs retained the antioxidant effect of Zingerone as assessed by DPPH scavenging assay. Evaluation of nanoformulation for anti-virulence potential against Pseudomonas aeruginosa depicted significant reduction in swimming, swarming, and twitching motilities along with quorum sensing inhibition and eradication of biofilms. Decrease in expression of quorum sensing (QS) genes was also observed in the presence of Z-NPs. The results of the present study revealed that Z-NPs could be exploited as a promising anti-virulence candidate against P. aeruginosa infections.


Author(s):  
Sunil K Jain ◽  
Vaibhav Dubey ◽  
Kuldeep Rajpoot

Colorectal cancer is one of the most familiar malignant tumor, which requires an efficient system specially fabricated for targeted delivery of anticancer agents. 5-Fluorouracil (5-FU) is mostly used as an antineoplastic agent in gastrointestinal cancer. Ligand-based targeting approaches increase the internalization of NPs within resistant cells, which results in highly well-organized treatment, markedly reduces systemic toxicities, and minimize collateral damage to adjacent healthy cells. Mannose-conjugation was carried out to increase its uptake by the cancer cells through receptor-mediated endocytosis. It was attempted to develop d-mannose conjugated 5-fluorouracil (5-FU) entrapped nanoparticles (NPs) with an objective to target colon cancer. The conjugated-NPs were characterized for distinct parameters, for instance, pH, viscosity, morphology of particles, particle size (PS), size-distribution, polydispersity index, %yield, surface charge, and entrapment efficiency. However, formulations were also examined (in vitro) for cell cytotoxicity against CT26 and drug leakage in dissolution fluid. The fabricated NPs produced sustained drug release effect and exhibited release of 5-FU for 24 h. In addition, conjugation of d-mannose with NPs significantly augmented sustained effect over non-conjugated formulations. The preliminary results obtained for this study suggested that conjugation of d-mannose with chitosan NPs augmented the targeting effect in colon cancer. In conclusion, d-mannose conjugated NPs proved to be a more efficient carrier system over other conventional formulation as a delivery system for tumor.


2011 ◽  
Vol 106 (9) ◽  
pp. 1330-1336 ◽  
Author(s):  
Wei-Lin Liu ◽  
Wei Liu ◽  
Cheng-Mei Liu ◽  
Shui-Bing Yang ◽  
Jian-Hua Liu ◽  
...  

Medium-chain fatty acids (MCFA) are widely used in diets for patients with obesity. To develop a delivery system for suppressing dietary fat accumulation into adipose tissue, MCFA were encapsulated in nanoliposomes (NL), which can overcome the drawbacks of MCFA and keep their properties unchanged. In the present study, crude liposomes were first produced by the thin-layer dispersion method, and then dynamic high-pressure microfluidisation (DHPM) and DHPM combined with freeze–thawing methods were used to prepare MCFA NL (NL-1 and NL-2, respectively). NL-1 exhibited smaller average size (77·6 (sd 4·3) nm), higher zeta potential ( − 40·8 (sd 1·7) mV) and entrapment efficiency (73·3 (sd 16·1) %) and better stability, while NL-2 showed narrower distribution (polydispersion index 0·193 (sd 0·016)). The body fat reduction property of NL-1 and NL-2 were evaluated by short-term (2 weeks) and long-term (6 weeks) experiments of mice. In contrast to the MCFA group, the NL groups had overcome the poor palatability of MCFA because the normal diet of mice was maintained. The body fat and total cholesterol (TCH) of NL-1 (1·54 (sd 0·30) g, P = 0·039 and 2·33 (sd 0·44) mmol/l, P = 0·021, respectively) and NL-2 (1·58 (sd 0·69) g, P = 0·041 and 2·29 (sd 0·38) mmol/l, P = 0·015, respectively) significantly decreased when compared with the control group (2·11 (sd 0·82) g and 2·99 (sd 0·48) mmol/l, respectively). The TAG concentration of the NL-1 group (0·55 (sd 0·14) mmol/l) was remarkably lower (P = 0·045) than the control group (0·94 (sd 0·37) mmol/l). No significant difference in weight and fat gain, TCH and TAG was detected between the MCFA NL and MCFA groups. Therefore, MCFA NL could be potential nutritional candidates for obesity to suppress body fat accumulation.


2020 ◽  
Vol 15 ◽  
Author(s):  
Manasi M. Chogale ◽  
Sujay S. Gaikwad ◽  
Savita P. Kulkarni ◽  
Vandana B. Patravale

Background: Tuberculosis (TB) continues to be among the leading causes for high mortality among developing countries. Though a seemingly effective treatment regimen against TB is in place, there has been no significant improvement in the therapeutic rates. This is primarily owing to the high drug doses, their associated sideeffects, and prolonged treatment regimen. Discontinuation of therapy due to the severe side effects of the drugs results in the progression of the infection to the more severe drug-resistant TB. Objectives: Reformulation of the current existing anti TB drugs into more efficient dosage forms could be an ideal way out. Nanoformulations have been known to mitigate the side effects of toxic, high-dose drugs. Hence, the current research work involves the formulation of Isoniazid (INH; a first-line anti TB molecule) loaded chitosan nanoparticles for pulmonary administration. Methods: INH loaded chitosan nanoparticles were prepared by ionic gelation method using an anionic crosslinker. Drugexcipient compatibility was evaluated using DSC and FT-IR. The formulation was optimized on the principles of Qualityby-Design using a full factorial design. Results: The obtained nanoparticles were spherical in shape having an average size of 620±10.97 nm and zeta potential +16.87±0.79 mV. Solid state characterization revealed partial encapsulation and amorphization of INH into the nanoparticulate system. In vitro release study confirmed an extended release of INH from the system. In vitro cell line based safety and efficacy studies revealed satisfactory results. Conclusion: The developed nanosystem is thus an efficient approach for antitubercular therapy.


2020 ◽  
Vol 14 (3) ◽  
pp. 210-224
Author(s):  
Gayatri Patel ◽  
Bindu K.N. Yadav

Background: The purpose of this study was to formulate, characterize and in-vitro cytotoxicity of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection polymers and method for the preparation of nanoparticles. Methods: In the present study nanoparticles were prepared by simple ionic gelation method using various concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and drug release study. Results: The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1 nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy and dynamic light scattering technique revealed spherical particles with uniform size. The invitro release profile showed controlled release up to 24 hr. Further study was carried using A375 basal cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay. Conclusion: These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell carcinoma type of skin cancer.


2019 ◽  
Vol 9 (2) ◽  
pp. 89-96
Author(s):  
Abbaraju Krishna Sailaja ◽  
Juveria Banu

Aim: The aim of this investigation was to develop and characterize naproxen loaded chitosan nanoparticles by emulsion interfacial reaction method. Methodology: For emulsion interfacial reaction method chitosan was used as a polymer. In this method, eight formulations were prepared by varying drug to polymer concentration. Discussion: Out of eight formulations prepared using emulsion interfacial reaction method EI8 formulation was found to be the best formulation. The drug content was observed as 94.4%, entrapment efficiency and loading capacity were found to be 87.5% and 75%, respectively. The mean particle diameter was measured as 324.6nm and the Zeta potential value was found to be -42.4mv. In vitro drug release data showed 97.2% of drug release rate sustained up to 12hrs. Conclusion: The results clearly reveal that EI8 formulation having the highest amount of drug was considered as the best formulation because of its small mean particle diameter, good entrapment efficiency, and stability.


Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 677
Author(s):  
Sara A. Abosabaa ◽  
Aliaa N. ElMeshad ◽  
Mona G. Arafa

The objective of the present research is to propose chitosan as a nanocarrier for caffeine—a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared via the ionic gelation technique and optimized according to a Box–Behnken design. The effect of (A) chitosan concentration, (B) chitosan solution pH, and (C) chitosan to sodium tripolyphosphate mass ratio on (Y1) entrapment efficiency percent, (Y2) particle size, (Y3) polydispersity index, and (Y4) zeta potential were studied. Subsequently, the desired constraints on responses were applied, and validation of the optimization procedure was confirmed by the parameters exhibited by the optimal formulation. A caffeine entrapment efficiency percent of 17.25 ± 1.48%, a particle size of 173.03 ± 4.32 nm, a polydispersity index of 0.278 ± 0.01, and a surface charge of 41.7 ± 3.0 mV were attained. Microscopical evaluation using transmission electron microscope revealed a typical spherical nature of the nanoparticles arranged in a network with a further confirmation of the formation of particles in the nano range. The results proved the successful implementation of the Box–Behnken design for optimization of chitosan-based nanoparticles in the field of advanced polymeric systems for pharmaceutical and cosmeceutical applications.


Coatings ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 435
Author(s):  
Reham Z. Hamza ◽  
Mohammad S. Al-Harbi ◽  
Munirah A. Al-Hazaa

Aging is a neurological disease that is afforded by incidence of oxidative stress. Chitosan has received global interests due to its wide medical uses. Quercetin (Q) is a bioflavonoid and widely distributed in vegetables and fruits. Resveratrol is considered as a potent antioxidant and is a component of a wide range of foods. The using of either chitosan nanopartciles (CH-NPs), querectin (Q), and resveratrol (RV) to reduce the oxidative stress and biochemical alterations on brain and testicular tissues induced by D-galactose (DG) (100 mg/Kg) were the aim of the present study. This study investigated the probable protective effects of CH-NPs in two doses (140,280 mg/Kg), Q (20 mg/Kg) and RV (20 mg/Kg), against DG induced aging and neurological alterations. Brain antioxidant capacity as malonaldehyde (MDA), catalase (CAT), and glutathione reductase (GRx), as well as histopathological damages of the brain and testicular tissues were measured. The DG treated group had significantly elevated the oxidative stress markers by 96% and 91.4% in brain and testicular tissues respectively and lower significantly the antioxidant enzyme activities of both brain and testicular tissues than those of the control group by 86.95%, 69.27%, 83.07%, and 69.43%. Groups of DG that treated with a combination of CH-NPs in two doses, Q and RV, the levels of oxidative stress marker declined significantly by 68.70%, 76.64% in brain tissues and by 74.07% and 76.61% in testicular tissues, and the enzymatic antioxidants increased significantly by 75.55%, 79.24%, 62.32%, and 61.97% as compared to the DG group. The present results indicate that CH-NPs, Q, and RV have protective effects against DG-induced brain and testis tissue damage at the biochemical and histopathological levels. Mechanisms of this protective effect of used compounds against neurological and testicular toxicity may be due to the enhanced brain and testis antioxidant capacities.


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