Development and Evaluation of Lycopene Loaded Chitosan Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 61-75 ◽  
Author(s):  
A. Dhiman ◽  
D. Bhalla
Keyword(s):  
Sodium Tripolyphosphate ◽  
Polymeric Nanoparticles ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
Great Promise ◽  
Scanning Calorimetry ◽  
Stirring Time

Background: Nanotechnology has gained a great deal of public interest due to the needs and applications of nanomaterials in many areas of human endeavours such as industry, agriculture, business, medicine and public health amongst many others. Polymeric nanoparticles from biodegradable and biocompatible polymers are good candidates for drug carrier to deliver the drugs because they are expected to be adsorbed in an intact form in the gastrointestinal tract after oral administration. Objective: The objective of the study was to investigate the influence of some precarious variables like, concentration of chitosan, concentration of sodium tripolyphosphate (STPP) and stirring time on physicochemical characteristics of lycopene loaded chitosan nanoparticles. Method: Eight batches of lycopene loaded chitosan nanoparticles were prepared using various concentrations of chitosan (100-200 mg), STPP (50-100 mg) by varying stirring speed in the range of 10-20 minutes using ionic gelation method. The optimized nanoparticulate formulation was characterized for various parameters like morphology study, particle size and size distribution studies, differential scanning calorimetry, entrapment efficiency and in-vitro drug release studies. Results: Lycopene loaded chitosan nanoparticles containing 150 mg of chitosan, 75 mg of STPP, 20 mg of drug lycopene and with 15 min of stirring time showed entrapment efficiency of 89.4%. The percent release of lycopene loaded chitosan nanoparticles at the end of 6 h was found to be 83.5%, however, percent release of pure lycopene at the end of 6 h was observed as 79.6%. Conclusion: Lycopene loaded chitosan nanoparticles may show a great promise for the development of drug delivery system by enhancing the cellular accumulation of lycopene with chitosan.

scholarly journals FORMULATION OPTIMIZATION AND CHARACTERIZATION OF GANCICLOVIR LOADED DRY CHITOSAN NANOPARTICLES

2017 ◽  
Vol 10 (3) ◽  
pp. 295 ◽  
Author(s):  
Gayatri Patel ◽  
Rutu Patel ◽  
Balaram Gajra ◽  
R. Parikh
Keyword(s):  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Interactive Effects ◽  
Physicochemical Interaction ◽  
Ionic Gelation ◽  
Scanning Calorimetry ◽  
Box Behnken Design ◽  
The Matrix ◽  
Stirring Time

ABSTRACTObjective: The objective of this work was to formulate, optimize, and characterize ganciclovir (GCV) loaded dry chitosan nanoparticles (CSNPs).Methods: The GCV loaded CSNPs was prepared by ionic gelation method. Box–Behnken design was employed to optimize the influence of independentprocess and formulation variables like drug to polymer ratio, concentration of sodium tripolyphosphate, and stirring time (min) on the dependentvariables such as particle size (PS) and drug encapsulation efficiency (% EE). The optimum conditions were determined by regression analysis of theoutput data.Results: The independent variables had interactive effects and they affected both the responses. The optimum formulation had PS within the range of100-120 nm and % EE between 85% and 86%. The prepared GCV loaded CSNPs were dried by fluidized bed drying method. Fourier transform infraredspectra showed there was no physicochemical interaction between GCV and CS. Powder X-ray diffraction study showed less intense crystalline peaksindicated that GCV may exist in the formulation as amorphous nanodispersion or molecular dispersion form. Differential scanning calorimetry studywas performed which indicated that the drug was molecularly dispersed inside the matrix of CS. Higuchi model was the best to fit the in vitro releasedata for the GCV loaded CSNPs.Conclusion: From the results, it can be concluded that the GCV loaded dry CSNPs were formulated, optimized, and characterized using desiredpharmacotechnical properties.Keywords: Chitosan nanoparticles, Box–Behnken design, Sodium tripolyphosphate, Ionic gelation.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

2021 ◽  
pp. 120-125
Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Release Kinetics ◽  
Ph Effect ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Mode Of Delivery ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Novel Approach

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.

Preparation, Characterization, and In Vitro Evaluation of EGCG-Loaded Chitosan Nanoparticles

2011 ◽  
Vol 282-283 ◽  
pp. 539-544 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Zhi Gang An ◽  
Xiao Yu Sui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery Systems ◽  
Room Temperature ◽  
Active Component ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Release Drug

Epigallocatechin-3-gallate (EGCG), a principal polyphenolic, which is most abundant and active component in tea. It is considered key to these healthful qualities. However, EGCG used in clinical application which is still shortcomings of short half-life and low bioavailability. Chitosan (CS) has been widely used in pharmaceutical and medical areas, particularly for its potential in the development of controlled release drug delivery systems due to its well properties. In this study, we prepared EGCG-loaded chitosan nanoparticles by ionic polymeric method using sodium tripolyphosphate(TPP) as ionic polymeric agent successfully. Results controlled conditions (concentration of CS, 2 mg/mL; pH = 5.4; volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min))volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min)) for entrapment efficiency, loading efficiency, mean particle size and Zeta potential, were found to be 62.3 %, 33.8 %, 141.5 ± 0.4 nm and -31.21 ± 0.54 mV, respectively, and CS-EGCG-NPS have well property of sustained release.

scholarly journals Preparation and Characterization of Curcumin Loaded Dextrin Sulfate- Chitosan Nanoparticles for Promoting Curcumin Anticancer Activity

2019 ◽  
Vol 16 (1) ◽  
pp. 185-195
Author(s):  
Nihal S Elbialy
Keyword(s):  
Cancer Cells ◽  
Polymeric Nanoparticles ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Hydrodynamic Diameter ◽  
Transmission Electron ◽  
Hct 116 ◽  
Nano Formulation

Curcumin as a natural medicinal agent has been proved to kill cancer cells effectively. However, its biomedical applications have been hindered owing to its poor bioavailability. Many nanoparticulate systems have been introduced to overcome this problem. Among this types polymeric-based nanoparticles which exhibit unique properties allowing their use as a efficient drug carrier. Developing a polymeric- blend nanoparticles will offer a promising nanocarrier with excellent biocompatibility, biodegradability and low immunogencity. In this study, curcumin nano-vehicle has been made up by combining dextren sulfate and chitosan (DSCSNPs). DSCSNPs have been characterized using different techniques. Transmission electron microscopy (TEM) which revealed the spherical, smooth surface of the nano-formulation. Dynamic light scattering (DLS) for measuring DSCSNPs hydrodynamic- diameter. Zeta potential measurements showed nanoparticles high stability. Fourier transform infrared spectroscopy (FTIR) confirmed  successful combination between the two polymers and curcumin loading on naoparticles surface. Curcumin release profile out of DSCSNPs showed high drug release in tumor acidic microenvironment. In vitro cytotoxicity measurements demonstrated that curcumin loaded polymeric nanoparticles (DSCSNPs-Cur) have high therapeutic efficacy against colon (HCT-116) and breast  (MCF-7) cancer cells compared with free curcumin.  DSCSNPs as a combined biopolymers is an excellent candidate for improving curcumin bioavailability  allowing its use as anticancer  agent.

scholarly journals Formulation and Characterization of gallic acid and quercetin chitosan nanoparticles for sustained release in treating Colorectal Cancer

2021 ◽  
Author(s):  
Poournima Patil ◽  
Suresh Killedar
Keyword(s):  
Colorectal Cancer ◽  
Gallic Acid ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Aberrant Crypt Foci ◽  
Spectroscopic Techniques ◽  
X Ray Diffraction ◽  
Scanning Calorimetry

Abstract The current work was addressed to characterize gallic acid from amla fruit and quercetin from peels of pomegranate fruit and formulated into Chitosan (CS) nanoparticles and to evaluate their cytotoxicity towards human colorectal cancer (HCT 116) cell lines for the treatment of DMH induced colorectal cancer in Wistar rats. Identification of the biomolecules was performed by using different chromatographic and spectroscopic techniques, as 1H-NMR, GC-MS, LC-MS and HPTLC. Characterization of CS nanoparticles carried out by using X- ray diffraction (XRD) Differential scanning calorimetry (DSC), Scanning Electron Microscope (SEM), entrapment efficiency and In vitro drug release confirmed successful encapsulation of biomolecules into CS nanoparticles. A significant change in aberrant crypt foci (ACF) in CS nanoparticles compared to polyherbal extract were observed, with decrease in the colonic glutathione, catalase and superoxide dismutase levels and values differed significantly (P < 0.005).

scholarly journals Formulation and In-Vitro Characterization of Chitosan-Nanoparticles Loaded with the Iron Chelator Deferoxamine Mesylate (DFO)

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 238 ◽  
Author(s):  
Maria Lazaridou ◽  
Evi Christodoulou ◽  
Maria Nerantzaki ◽  
Margaritis Kostoglou ◽  
Dimitra Lambropoulou ◽  
...  
Keyword(s):  
Sodium Tripolyphosphate ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Release Mechanism ◽  
Hydroxyl Groups ◽  
Deferoxamine Mesylate ◽  
Pharmacologically Active

The objective of this study was to develop chitosan (CS) nanoparticles (NPs) loaded with deferoxamine mesylate (DFO) for slow release of this iron-chelating drug. Drug nanoencapsulation was performed via ionic gelation of chitosan using sodium tripolyphosphate (TPP) as cross-linker. Nanoparticles with a size ranging between 150 and 400 nm were prepared for neat CS/TPP with a 2/1 molar ratio while their yield was directly dependent on the applied stirring rate during the preparation process. DFO at different content (20, 45 and 75 wt %) was encapsulated into these nanoparticles. We found that drug loading correlates with increasing DFO content while the entrapment efficiency has an opposite behavior due to the high solubility of DFO. Hydrogen-bonding between amino and hydroxyl groups of DFO with reactive groups of CS were detected using FT-IR spectroscopy while X-ray diffraction revealed that DFO was entrapped in amorphous form in the CS nanoparticles. DFO release is directly dependent on the content of loaded drug, while model analysis revealed that the release mechanism of DFO for the CS/TPP nanoparticles is by diffusion. Treatment of murine RAW 264.7 macrophages with nanoencapsulated DFO promoted an increased expression of transferrin receptor 1 (TfR1) mRNA, a typical homeostatic response to iron deficiency. These data provide preliminary evidence for release of pharmacologically active DFO from the chitosan nanoparticles.

Chondroitin Sulphate Decorated Polymeric Nanoparticles: An Effective Carrier for Enhancement of Lung Cancer Targeting Capabilities of Anticancer Drug

2019 ◽  
Vol 9 (3) ◽  
pp. 243-261 ◽  
Author(s):  
Sweta Garg ◽  
Ashish Garg ◽  
Sreenivas Enaganti ◽  
Awesh K. Yadav
Keyword(s):  
Lung Cancer ◽  
Anticancer Drug ◽  
Chondroitin Sulphate ◽  
Polymeric Nanoparticles ◽  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Force Microscopy ◽  
A549 Cancer Cell Line

Background: Currently, cancer is rising as one of the dominant causes of human deaths worldwide. The application of nano-carriers may help to treat cancer through the delivery of anticancer drugs inside the tumor cells. Objective: The foremost objective behind this research was to formulate chondroitin sulfate tailored cellulose acetate phthalate (CSAC) core shield nanoparticles (NPs) containing 5-Fluorouracil (5-FU) as an anticancer drug. Methods: The FTIR and 1H-NMR spectroscopic methods were used to analyze and characterize the formulation of CSAC copolymer. NPs were typified by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), Atomic Force Microscopy (AFM), Entrapment efficiency and in-vitro drug release. Results: CSAC NPs were found to exhibit moderate release (95.59±0.15% in 34hrs) than CAP NPs (78.97±0.08% in 8 hours). In the course of cytotoxicity examination in A549 cancer cell line, the results revealed that these 5-FU loaded CSAC NPs showed an immense cytotoxic potentiality. Moreover, CSAC NPs exhibit least hemolytic activity when compared with CAP NPs and plain 5-FU. Conclusion: Conclusively, it was found that the CSAC NPs is an efficient carrier system for the better release of 5-FU in lung cancer.

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