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).

Colon Available Bioactive Compounds Exhibits Anticancer Effect on In-Vitro Model of Colorectal Cancer

2021 ◽  
Author(s):  
Poounima Patil ◽  
Suresh Killedar
Keyword(s):  
Colorectal Cancer ◽  
Gallic Acid ◽  
Hct116 Cell ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Spectroscopic Techniques ◽  
X Ray Diffraction ◽  
Hct 116 ◽  
Vitro Model

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. Identification of the biomolecules was performed by chromatographic and spectroscopic techniques and characterization of gallic acid and quercetin loaded chitosan nanoparticles carried out by using FT-IR, X- ray diffraction, entrapment efficiency and loading content confirmed successful encapsulation of biomolecules into nanoparticles. In vitro drug release studies done by using simulated fluids at various pH (1.2, 4.5, 7.5, and 7.0) to mimic the GIT tract and achieved drug releases 77.56% for gallic acid 79.06% for quercetin at 24 hr. in a sustained manner. The human HCT116 cell line by MTT assay results inferred that the synthesized CS nanoparticles demonstrated shows more effective antiproliferative potential with IC50 value of 36.17 ug/ml than polyherbal extract 60.32ug/ml.

Mannosylated Solid Lipid Nanocarriers Of Chrysin To Target Gastric Cancer: Optimization and Cell line Study.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya
Keyword(s):  
Gastric Cancer ◽  
Particle Size ◽  
Ex Vivo ◽  
Biological Effects ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Lipid Nanocarriers

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

scholarly journals FORMULATION ANDCHARACTERIZATION OF OLANZEPINELOADED MUCOADHESIVE MICROSPHERES

2017 ◽  
Vol 10 (4) ◽  
pp. 249
Author(s):  
Madhuri T Deshmukh ◽  
Shrinivas K Mohite
Keyword(s):  
Fourier Transforms ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Ionic Gelation ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Model Stability ◽  
X Ray ◽  
Mucoadhesive Microsphere

Objective: The objective of this research was to formulate and evaluate olanzapine (OLE) mucoadhesive microsphere prepared using carbopol and sodium combination. OLE having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation.Methods: OLE mucoadhesive microspheres were prepared by ionic gelation method. OLE mucoadhesive microspheres were prepared byionic gelation method by using calcium chloride as crosslinking agent. The OLE mucoadhesive microsphere was characterized by particle sizemeasurement, process yield, morphology of microsphere, drug entrapment efficiency, mucoadhesion test, differential scanning calorimetry, powder X-ray diffraction, Fourier transforms infrared (FTIR) study and in-vitro drug release.Results: The OLE mucoadhesive microsphere having mean particle size ranged from 546.0 µm to 554.3 µm, and the entrapment efficiencies ranged from 73% to 96%. All the olanzapine (OLE) microsphere batches showed good in-vitro mucoadhesive property ranging from 75.89% to 96.47% and in the in-vitro wash off test ranging from 68.12% to 81.3%. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F9. Therewere no compatibility issues, and the crystallinity of OLE was found to be reduced shoeing less intense peak in prepared mucoadhesive microspheres, which were confirmed by differential scanning calorimeter and X-ray diffraction studies. Among different formulations, the OLE microspheres of batch F9 had shown the optimum percent drug entrapment of microspheres. Release pattern of OLE from F9 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F9 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment, mucoadhesive behavior, and drug release were within permissible limits.Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of mucoadhesive microsphere.Keywords: Ionic gelation method, Gastroretentive delivery, Mucoadhesive microsphere, Carbopol.

Synergistic Antioxidant and Antibacterial Activity of Curcumin-C3 Encapsulated Chitosan Nanoparticles

2020 ◽  
Vol 26 (39) ◽  
pp. 5021-5029 ◽  
Author(s):  
Desu N.K. Reddy ◽  
Fu-Yung Huang ◽  
Shao-Pin Wang ◽  
Ramya Kumar
Keyword(s):  
Drug Release ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Antibacterial Activities ◽  
In Vitro Assays ◽  
X Ray Diffraction ◽  
Bacterial Diseases ◽  
Transmission Electron ◽  
Chitosan Nanoparticle

Background: Recent studies have focused on the nanoformulations of curcumin to enhance its solubility and bioavailability. The medicinal properties of curcumin-C3 complex, which is a combination of three curcuminoids (curcumin, demethoxycurcumin and bisdemethoxycurcumin) is less explored. Objective: The aim of this study was to prepare curcumin-C3 encapsulated in chitosan nanoparticles, characterize and evaluate their antioxidant and antibacterial potential. Methods: Ionic gelation method was used to prepare curcumin-C3 nanoparticles and was characterized by Fourier transform infrared spectroscopy, X-ray diffraction, transmission electron microscopy and nanoparticle tracking analysis. In vitro assays were performed to assess drug release, antioxidant and antibacterial activities. Results: Curcumin-C3-chitosan nanoparticle showed an increased entrapment efficiency of >90%, drug release and improved antioxidant potential. Moreover, curcumin-C3-chitosan nanoparticle showed stronger inhibition of Escherichia coli and Staphylococcus aureus. Conclusion: Chitosan is a suitable carrier for curcumin-C3 nanoparticle and can be used as a drug delivery system in the treatment of inflammatory and bacterial diseases.

A Logical Approach to Development of Natamycin Loaded NLCs: Preformulation Studies, Formulation Development and In Vitro Characterization

2021 ◽  
pp. 6033-6040
Author(s):  
Ishwari Choudhary ◽  
Preeti K. Suresh
Keyword(s):  
Entrapment Efficiency ◽  
Formulation Development ◽  
Visible Spectroscopy ◽  
Scanning Calorimetry ◽  
Solubility Profile ◽  
In Vitro Characterization ◽  
Uv Visible ◽  
Preformulation Studies

This study was aimed at the development of natamycin loaded nano-structured lipid carriers (NLCs) and their characterization for physicochemical properties i.e., Fourier Transform Infrared (FTIR), UV-Visible spectroscopy, meting point, solubility profile and partition coefficient. FTIR and Differential Scanning Calorimetry (DSC) permit the characterization of the drug, excipients and binary mixture and thus assisted in predicting the compatibility of natamycin with other excipients. Lipid screening for formulation of NLCs were performed by their solubility and drug affinity studies. High homogenization and sonication method was employed for the development of natamycin loaded NLCs and it was characterized for vesicle size, zeta potential, % entrapment efficiency, viscosity, pH and percentage drug release up to 12 h.

scholarly journals Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3139 ◽  
Author(s):  
Pradeep Kumar Bolla ◽  
Carlos A. Meraz ◽  
Victor A. Rodriguez ◽  
Isaac Deaguero ◽  
Mahima Singh ◽  
...  
Keyword(s):  
Fungal Infections ◽  
Entrapment Efficiency ◽  
Tape Stripping ◽  
X Ray Diffraction ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Topical Bioavailability ◽  
Diffusion Studies ◽  
Permeation Studies

Global incidence of superficial fungal infections caused by dermatophytes is high and affects around 40 million people. It is the fourth most common cause of infection. Clotrimazole, a broad spectrum imidazole antifungal agent is widely used to treat fungal infections. Conventional topical formulations of clotrimazole are intended to treat infections by effective penetration of drugs into the stratum corneum. However, drawbacks such as poor dermal bioavailability, poor penetration, and variable drug levels limit the efficiency. The present study aims to load clotrimazole into ufosomes and evaluate its topical bioavailability. Clotrimazole loaded ufosomes were prepared using cholesterol and sodium oleate by thin film hydration technique and evaluated for size, polydispersity index, and entrapment efficiency to obtain optimized formulation. Optimized formulation was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Skin diffusion studies and tape-stripping were performed using human skin to determine the amount of clotrimazole accumulated in different layers of the skin. Results showed that the optimized formulation had vesicle size <250 nm with ~84% entrapment efficiency. XRD and DSC confirmed the entrapment of clotrimazole into ufosomes. No permeation was observed through the skin up to 24 h following the permeation studies. Tape-stripping revealed that ufosomes led to accumulation of more clotrimazole in the skin compared to marketed formulation (Perrigo). Overall, results revealed the capability of ufosomes in improving the skin bioavailability of clotrimazole.

Synthesis and Characterization of SA-g-MAA Co-Polymer: Effect of Grafting and Process Variables on Controlled Release of an Anti-Bacterial Drug

2010 ◽  
Vol 123-125 ◽  
pp. 387-390 ◽  
Author(s):  
C.V. Prasad ◽  
K.M. Sudhan Rao ◽  
B. Mallikarjuna ◽  
M.C.S. Subha ◽  
K. Chowdoji Rao
Keyword(s):  
Sodium Alginate ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Potassium Persulphate ◽  
Preparation Conditions ◽  
Swelling Capacity ◽  
Release Profiles

Methacrylic acid (MAA) was grafted onto sodium alginate (SA) by thermal heating at ambient temperature (70±2OC) using potassium persulphate as an initiator (PPS). SA-g-MAA and pure sodium alginate beads were prepared and were characterized using Scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction techniques (X-Rd). The resultant products (SA-g-MAA) were used to prepare Glutaraldehyde (GA) crosslinked beads of various formulations by varying, monomer, cross-linker (GA) and drug content (CFHCl) in the graft co-polymer. Preparation conditions of the beads were optimized by considering the percentage entrapment efficiency, swelling capacity and release profiles. Release profile of CFHCl was discussed at 370C in a gastrointestinal atmosphere (pH -7.4 and acidic medium pH-1.2). It was observed that, CFHCl release from the beads increased with increasing MAA content over the entire studied range. As GA and CFHCl content increases, swelling ratio decreases resulting in decrease in the drug release rate. The highest CFHCl release was obtained to be 99% for the beads containing 40% monomer, 0.5mL GA and 10% CFHCl at pH-7.4. It was also observed that the release profiles have effect on pH and hence the graft co-polymeric beads can be used as pH sensitive drug devices.

scholarly journals Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility

2019 ◽  
Vol 28 (2) ◽  
pp. 124-133
Author(s):  
Asmaa M. Rashid ◽  
Shaimaa N. Abdal-Hammid
Keyword(s):  
Fourier Transforms ◽  
Fungal Infections ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Nanoprecipitation Method ◽  
Systemic Infections

Abstract             Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis,  and for the prophylaxis of fungal infections in immunocompromised patients.            The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.           Itraconazole nanosuspension was produced by a solvent-antisolvent nanoprecipitation method in the presence of different stabilisers (Poloxamer-188, HPMCE5) at different ratios with the drug alone or combination with surfactant(tween 80, SLS).          The results exhibit that the particle sizes of all prepared itraconazole formulations were in the nano size.  The best formula (F6) has a particle size.  ( 42  ) nm and Zeta potential of (- 21.86 ) mV.  In vitro cumulative release from the nanosuspension was (88 %) at (30) min when compared to the pure drug (13%) and lyophilized nanoparticles (98.2%) at (30)min. Effect of different parameters was investigated.           Fourier transforms infrared spectroscopy(FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction (XRD), Scanning electron microscope( SEM) was done for the optimized  nanoparticles prepared by lyophilization technique         Thus, Nanosuspension appears to be an encouraging approach to formulate Itraconazole nanosuspension with high solubility and dissolution rate.               Keywords: Itraconazole, Nanoprecipitation method, Nanosuspension          

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.

Sign in / Sign up

Export Citation Format

Share Document