scholarly journals Development of NIPAAm-PEG acrylate polymeric nanoparticles for co-delivery of paclitaxel with ellagic acid for the treatment of breast cancer

2019 ◽  
Vol 39 (3) ◽  
pp. 271-278 ◽  
Author(s):  
Suruchi Suri ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Abdullah S. Alshetaili ◽  
Saad M. Alshahrani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Ellagic Acid ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Shell Nanoparticles ◽  
Transmission Electron ◽  
Core Shell Nanoparticles

Abstract The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitro release profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.

scholarly journals Effect of Chitosan Coating on PLGA Nanoparticles for Oral Delivery of Thymoquinone: In Vitro, Ex Vivo, and Cancer Cell Line Assessments

Coatings ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 6
Author(s):  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Md Rizwanullah ◽  
Khalid Umar Fakhri ◽  
Mohd Moshahid Alam Rizvi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Cancer Management ◽  
Mcf 7

In the present study, thymoquinone (TQ)-encapsulated chitosan- (CS)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33-QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l-lactide-co-glycolide) nanoparticles (TQ-CS-PLGA-NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The surface coating of PLGA-NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ-CS-PLGA-NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ-PLGA-NPs and TQ-CS-PLGA-NPs. The optimized TQ-CS-PLGA-NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ-PLGA-NPs and TQ suspension. Furthermore, TQ-CS-PLGA-NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated TQ-PLGA-NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan-coated TQ-PLGA-NPs represent a great potential for breast cancer management.

scholarly journals Chitosan anchored nanoparticles for breast cancer: preparation and evaluation: part-I

2019 ◽  
Vol 9 (1) ◽  
pp. 1-5
Author(s):  
Rajkumari Thagele ◽  
Archana Bagre ◽  
Mohan Lal Kori
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Polymeric Nanoparticles ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
Physical Factors ◽  
Ionic Gelation ◽  
Shell Nanoparticles ◽  
Preparation And Evaluation

The objective of present research work was to develop methotrexate loaded chitosan anchored shell nanoparticles for drug delivery in breast cancer. Chitosan nanoparticles (CS-NPs) were synthesized by ionic gelation of chitosan using sodium tripolyphosphate (STPP). The optimized nanoparticles were characterized for particle size and polydispersity index (PDI) revealed particle size were found to be between 57.08 nm to169.5 nm and PDI 0.252 to 0.639 respectively. The results signpost that stirring speed during ionic gelation reaction was also decisive parameters for the size of the nanoparticles obtained. Further characterization involved to show polymer-drug interaction was FTIR and DSC. This paper grants a revision of the physical factors elaborate in attaining nanoparticles in order to regulate the particle size of polymeric nanoparticles made from chitosan, without any surplus chemical treatment. Keywords: Breast cancer, Nanoparticles, Chitosan, Methotrexate

scholarly journals BENAZEPRIL HYDROCHLORIDE LOADED NIOSOMAL FORMULATION FOR ORAL DELIVERY: FORMULATION AND CHARACTERIZATION

2018 ◽  
Vol 10 (5) ◽  
pp. 66
Author(s):  
Ameerah A. Radhi
Keyword(s):  
Zeta Potential ◽  
Oral Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Range ◽  
Transmission Electron ◽  
Study Results ◽  
Span 60 ◽  
A Charge

Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.

scholarly journals Chitosan Coated Luteolin Nanostructured Lipid Carriers: Optimization, In Vitro-Ex Vivo Assessments and Cytotoxicity Study in Breast Cancer Cells

Coatings ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 158
Author(s):  
Sadaf Jamal Gilani ◽  
May Bin-Jumah ◽  
Md. Rizwanullah ◽  
Syed Sarim Imam ◽  
Khalid Imtiyaz ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Cell Lines ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Breast Cancer Cell Lines ◽  
Cancer Management ◽  
Mcf 7

In the present study, luteolin (LTN)-encapsulated chitosan (CS) coated nanostructured lipid carriers (NLCs) were formulated using the melt emulsification ultrasonication technique. NLCs were optimized by using the 33-QbD approach for improved in vitro efficacy against breast cancer cell lines. The optimized LTN-CS-NLCs were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The prepared LTN-CS-NLCs showed particle size (PS), polydispersity index (PDI), and entrapment efficiency (%EE) in the range between 101.25 nm and 158.04 nm, 0.11 and 0.20, and 65.55% and 95.37%, respectively. Coating of NLCs with CS significantly increased the particle size, encapsulation efficiency, and zeta potential changes positively. Moreover, slow-release rate of LTN was achieved during 24 h of study for LTN-CS-NLCs. In addition, optimized LTN-CS-NLCs showed significantly higher mucoadhesion, gastrointestinal stability, and intestinal permeation compared to non-coated LTN-NLCs and LTN suspension. Furthermore, LTN-CS-NLCs showed statistically enhanced antioxidant potential as well as dose and time-dependent cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated LTN-NLCs and pure LTN. On the basis of the above findings, it may be stated that chitosan-coated LTN-NLCs represents a great potential for breast cancer management.

Mixed Micelles with Galactose Ligands for the Oral Delivery of Berberine to Enhance Its Bioavailability and Hypoglycemic Effects

2020 ◽  
Vol 16 (12) ◽  
pp. 1755-1764
Author(s):  
Hao Kang ◽  
Yingshui Yao ◽  
Xingwang Zhang
Keyword(s):  
Particle Size ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Mixed Micelles ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Profile ◽  
Sustained Drug Release ◽  
Oral Pharmacokinetics ◽  
Medical Relief

Diabetes mellitus (DM) has become an epidemic disorder that is an escalating public health risk. Currently, DM treatment is highly challenging due to temporary medical relief rather than a permanent cure. This article reports a ligand-anchored mixed micellar system formed by phospholipids and N -oleoyl-D-galactosamine aiming to enhance the oral bioavailability and hypoglycemic effects of berberine, an antidiabetic agent with poor absorption. Berberine-loaded mixed micelles (BBMMs) were prepared through a solvent diffusion technique. The resulting BB-MMs were characterized by particle size, potential, morphology, entrapment efficiency (EE) and in vitro release. The oral pharmacokinetics and hypoglycemic efficacy of BB-MMs were evaluated in rats and compared with a berberine suspension. As a result, BB-MMs prepared with the preferable formulation had a particle size of approximately 100 nm with an EE of over 85%. BB-MMs exhibited sustained drug release owing to the entrapment in the micelles. After oral administration, BB-MMs ameliorated the pharmacokinetic profile of berberine and significantly enhanced its oral bioavailability (317.17% relative to the suspension). The pharmacological effect (PE) of BB-MMs was approximately 3.44 times greater than that of the suspension. In addition, in situ single-pass intestinal perfusion and cellular testing results illustrated that BB-MMs had good intestinal permeability and cellular uptake. Our findings demonstrate that the oral bioavailability and hypoglycemic effects of berberine could be largely enhanced by encapsulation into mixed micelles with a galactose moiety. Thus, galactosylated micelles may be promising for developing berberine nanomedicines to fight DM.

Preparation and characterization of nanoparticles composed of methylated N-(4-N,N-dimethyl aminobenzyl) chitosan for oral delivery of cyclosporine A

2016 ◽  
Vol 8 (2) ◽  
Author(s):  
Reza Mahjub ◽  
Robabeh Allahyar ◽  
Morteza Rafiee-Tehrani ◽  
Farid Abedin Dorkoosh
Keyword(s):  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Chemical Properties ◽  
Simulated Intestinal Fluid ◽  
Equal Concentration ◽  
Prepared Nanoparticles ◽  
Transmission Electron ◽  
Physico Chemical

AbstractCyclosporine is considered a highly lypophilic compound meaning low bioavailability through oral administration. In this study, cyclosporine was entrapped in a novel aromatic, quaternized derivative of chitosan (i.e. methylated N-(4-N,N-dimethyl aminobenzyl) chitosan) in order to improve solubility and bioavailability. Methylated N-(4,N,N-dimethyl aminobenzyl) chitosan was synthesized by the Schiff base reaction method. Polymeric nanoparticles containing cyclosporine was prepared and the physico-chemical properties of prepared nanoparticles were determined. The nanoparticles were studied morphologically using transmission electron microscopy (TEM). Finally, the release of cyclosporine from nanoparticles was studied in vitro using simulated intestinal fluid adjusted to pH of 6.8. For the preparation of nanoparticles, different formulations were studied and it was found that proper nanoparticles were prepared in equal concentration (1 mg/mL) of polymer and sodium tri-poly phosphate (TPP). The size, zeta potential, PdI, EE% and LE% of the prepared nanoparticles were reported as 173±36 nm, 23.1±4.18 mV, 0.243±0.05, 97.1±4.38% and 3.2±0.21%, respectively. The TEM images of nanoparticles revealed spherical to sub-spherical nanoparticles with no sign of agglomeration. This study suggests that preparations of nanoparticles composed of methylated N-(4,N,N-dimethyl aminobenzyl) chitosan can be a good candidate for improving the oral bioavailability of cyclosporine.

scholarly journals FORMULATION, OPTIMIZATION, AND IN VITRO EVALUATION OF POLYMERIC NANOSUSPENSION OF FLURBIPROFEN

2019 ◽  
pp. 183-191
Author(s):  
PANKAJ JADHAV ◽  
ADHIKRAO YADAV
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Transmission Electron

Objective: At present, more than 40% of drugs are poorly water-soluble that leads to reduced bioavailability. The objective of the present investigation was to overcome the issue of poor aqueous solubility of drug; therefore, stable flurbiprofen (FBF) nanosuspensions were developed by nanoprecipitation method. Materials and Methods: Based on particle size, zeta potential, and entrapment efficiency, the polymeric system of hydroxypropyl methylcellulose E15 and poloxamer 188 was used effectively. The prepared formulations were evaluated for Fourier transform infrared spectroscopy, transmission electron microscopy, differential scanning calorimetry, powder X-ray diffraction, saturation solubility, entrapment efficiency, particle size, zeta potential, dissolution profile, and stability. Results: The resultant FBF nanosuspensions depicted particles in size range of 200–400 nm and were physically stable. After nanonization, the crystallinity of FBF was slightly reduced in the presence of excipients. The aqueous solubility and dissolution rate of all FBF nanosuspensions were significantly increased as compared with FBF powder. Conclusion: This investigation demonstrated that nanoprecipitation is a promising method to develop stable polymeric nanosuspension of FBF with significant increase in its aqueous solubility.

scholarly journals Nanoparticles made of multi-block copolymer of lactic acid and ethylene glycol containing periodic side-chain carboxyl groups for oral delivery of cyclosporine A

2010 ◽  
Vol 7 (suppl_4) ◽  
Author(s):  
D. D. Ankola ◽  
A. Battisti ◽  
R. Solaro ◽  
M. N. V. Ravi Kumar
Keyword(s):  
Molecular Weight ◽  
Particle Size ◽  
Lactic Acid ◽  
Block Copolymer ◽  
Ethylene Glycol ◽  
Cyclosporine A ◽  
Oral Delivery ◽  
Entrapment Efficiency

The purpose of this study was to evaluate the potential of new carboxylated multi-block copolymer of lactic acid and ethylene glycol (EL14) for nanoparticle (NP) formation and their ability to deliver high molecular weight hydrophobic drug—cyclosporine A (CsA). CsA-loaded EL14 NPs were compared with traditional poly(lactide-co-glycolide) (PLGA) NPs, both prepared by emulsion–diffusion–evaporation process. On the one hand, the increase in drug payload from 10 to 30 per cent for EL14 NPs showed no difference in particle size, however the entrapment efficiency tends to decrease from 50 to 43 per cent; on the other hand, the more hydrophobic PLGA showed an increasing trend in entrapment efficiency from 20 to 62 per cent with increasing particle size. Over 90 per cent of CsA was released in vitro from both the nanoparticulates; however, the release was much slower in the case of more hydrophobic PLGA. On in vivo evaluation in rats, the NPs made of EL14 showed a higher C max , a faster T max and enhanced tissue levels to that of PLGA that are crucial for CsA's activity and toxicity; however, the overall bioavailability of the nanoparticulates was similar and higher than Neoral. Together these data demonstrate the feasibility of NPs made of low molecular weight, hydrophilic polymer EL14 for efficient delivery of CsA.

scholarly journals Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine

Materials ◽  
2021 ◽  
Vol 14 (19) ◽  
pp. 5759
Author(s):  
Hussam I. Kutbi ◽  
Hani Z. Asfour ◽  
Ahmed K. Kammoun ◽  
Alaa Sirwi ◽  
Simona Cavalu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Water Solubility ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Structural Features ◽  
Transmission Electron ◽  
Mean Size ◽  
Therapeutic Activities

Various perspectives had been utilized to enhance the poor intestinal permeability and bioavailability of drugs with low water solubility. Berberine (Brb) is a unique molecule that possesses multiple therapeutic activities such as antimicrobial, anti-inflammatory, antioxidant and anti-hyperglycemic effects. To improve Brb permeability and bioavailability, this study presents a newly developed formulation, namely Brb hyaluronate-based liposomes, prepared by using film hydration method and characterized by dynamic light scattering measurements, entrapment efficiency percentage (EE%), transmission electron microscope (TEM), in vitro drug release and physical stability. The bioavailability of the selected formulations was assessed in vivo after oral administration to rats. The results revealed an enhanced effect of hyaluronic acid on the entrapment efficiency, reaching 78.1 ± 0.1% with mean size 520.7 ± 19.9 nm. Sustained release of Brb was recorded up to 24 h in comparison to Brb solution. Physical stability was maintained for three months at refrigeration temperature. Results of pharmacokinetics studies indicated the potential of the liposomal formulation to increase the oral bioavailability of Brb and to accelerate its entry into the bloodstream. The obtained results are accredited to the lipophilic nature of the prepared system, resembling the structural features of bio-membrane, in addition to their small size that enhances intestinal penetration.

scholarly journals Development and in vitro evaluation of Letrozole loaded biodegradable nanoparticles for breast cancer therapy

2009 ◽  
Vol 45 (3) ◽  
pp. 585-591 ◽  
Author(s):  
Sanjoy Kumar Dey ◽  
Bivash Mandal ◽  
Manas Bhowmik ◽  
Lakshmi Kanta Ghosh
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Cancer Therapy ◽  
Methylene Chloride ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Breast Cancer Therapy ◽  
Mean Size ◽  
High Entrapment Efficiency

The objectives of our study were to prepare and evaluate a biodegradable nanoparticulate system of Letrozole (LTZ) intended for breast cancer therapy. LTZ loaded poly(lactide-co-glycolide) nanoparticles (LTZ-PLGA-NPs) were prepared by emulsion-solvent evaporation method using methylene chloride and polyvinyl alcohol. Percentage of drug (with respect to polymer) was selected as formulation variable. LTZ-PLGA-NPs were characterized by particle size, zeta potential, infrared spectra, drug entrapment efficiency and in vitro release. Sonication was done with an ultrasound pulse sonicator at 70 W, 30 kHz for 90 sec to produce stable NPs of mean size range from 64 nm to 255 nm with high entrapment efficiency (68% to 82%). Percentage of drug significantly influenced particle size, entrapment efficiency and release (p <0.05). The system sustained release of LTZ significantly and further investigation could exhibit its potential usefulness in breast cancer therapy.

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