Preparation and Characterization of Chitosan Coated PLGA Nanoparticles of Resveratrol: Improved Stability, Antioxidant and Apoptotic Activities in H1299 Lung Cancer Cells

Resveratrol (RES) is a polyphenolic compound which has shown beneficial pharmacological effects such as anti-inflammatory, antioxidant, and anti-cancer effects. However, poor aqueous solubility, bioavailability, and low stability are the major limitations to the clinical application of RES. Therefore, in the present study, chitosan (CS) coated PLGA nanoparticles of RES (CS-RES-PLGA NPs) was developed, characterized and its anticancer activity was evaluated in the H1299 lung carcinoma cell line. The effects of the increase in CS coating and cryoprotectant concentration on particle size, polydispersity index (PDI) and zeta potential (ZP) were determined. The particle size, PDI, ZP and entrapment efficiency of the optimized CS-RES-PLGA NPs were found to be 341.56 ± 7.90 nm, 0.117 ± 0.01, 26.88 ± 2.69 mV and 75.13% ± 1.02% respectively. The average particle size and ZP showed a steady increase with an increase in CS concentration. The increase in positive zeta potential is evident for higher CS concentrations. The effect of trehalose as cryoprotectant on average particle size was decreased significantly (p < 0.05) when it was increased from 1%−5% w/v. TEM and SEM showed uniform particle distribution with a smooth surface and spherical shape. The CS coating provides modulation of in vitro drug release and showed a sustained release pattern. The stability of RES loaded PLGA NPs was improved by CS coating. CS-coated NPs showed greater cytotoxicity and apoptotic activities compared to free RES. The CS coated NPs had a higher antioxidant effect than the free RES. Therefore, CS coated PLGA NPs could be a potential nanocarrier of RES to improve drug solubility, entrapment, sustain release, stability and therapeutic application.

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DERMAL DELIVERY OF DOCETAXEL LOADED NANO LIQUID CRYSTALS FOR THE TREATMENT OF SKIN CANCER

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i5.34621 ◽

2019 ◽

pp. 188-193 ◽

Cited By ~ 1

Author(s):

ARTI MAJUMDAR ◽

NIDHI DUBEY ◽

NITIN DUBEY

Keyword(s):

Liquid Crystals ◽

Skin Cancer ◽

Zeta Potential ◽

Average Particle Size ◽

Entrapment Efficiency ◽

Cell Uptake ◽

Diffusion Method ◽

Average Particle ◽

Uptake Study

Objective: The aim of the present study is to develop docetaxel-loaded nano liquid crystals (NLCs) to enhanced and effective delivery of the drug to the skin cancer. Methods: NLCs bearing docetaxel were prepared by an emulsification solvent diffusion method. The formulated NLCs were characterized for average particle size, polydispersity index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations were studied for it's in vitro cell line and cell uptake study. Results: It was revealed that the average size of NLCs was found 178.3±5.07, PDI was 0.189, percent entrapment efficiency was found 71.3±2.49 and Zeta potential was found-17.3±2.4. In vitro release determined by Franz diffusion cell was found 61.6±3.2% after 72 hr. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay shows that Docetaxel loaded NLCs were giving more cytotoxicity as compared to the plain drug. The cell uptake study was found enhanced uptake of fluorescein isothiocyanate (FITC) loaded NLCs in comparison to plain FITC. Docetaxel and docetaxel-loaded NLCs showed 28.3±0.3 and 39.3±1.3 growth inhibition respectively after 48h upon incubation at 0.5 µg/ml concentration (p<0.05). Conclusion: The result of the studies was concluded that NLCs can be used as impending drug delivery system which may enhance the drug uptake and maintain the drug level for longer period of time and it is potential carrier system which can be used for the treatment of skin diseases like cancer.

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Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i43a32461 ◽

2021 ◽

pp. 24-36

Author(s):

Nilesh S. Kulkarni ◽

Mukta A. Kulkarni ◽

Rahul H. Khiste ◽

Mohini C. Upadhye ◽

Shashikant N. Dhole

Keyword(s):

Particle Size ◽

Drug Release ◽

Ethyl Cellulose ◽

Polymer Concentration ◽

Average Particle Size ◽

Entrapment Efficiency ◽

Vigna Mungo ◽

Average Particle ◽

Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

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Investigation on the Preparation, Characteristics, and Controlled Release Model of Paeonol-Loaded Liposome in Carbomer Hydrogel

Current Drug Delivery ◽

10.2174/1567201817666200115163506 ◽

2020 ◽

Vol 17 (2) ◽

pp. 159-173

Author(s):

Qinqin Liu ◽

Hongmei Xia ◽

Yinxiang Xu ◽

Yongfeng Cheng ◽

Zhiqing Cheng

Keyword(s):

Particle Size ◽

Controlled Release ◽

Average Particle Size ◽

Entrapment Efficiency ◽

Average Particle ◽

Filtration Method ◽

Ethanol Injection ◽

Soybean Phospholipid ◽

Release Model

Objective: Paeonol is a phenolic compounce that is volatile. In order to decrease its volatility and achieve controlled release, paeonol-loaded liposome in carbomer hydrogel was prepared by coating with soybean phospholipid via ethanol injection method and then added into the carbomer hydrogel. Methods: The quality of paeonol-loaded liposome in carbomer hydrogel was evaluated by the degree of roundness, particle size distribution, zeta potential, entrapment efficiency (filtration method and chitosan neutralization method), viscosity, infrared spectrum, etc. Furthermore, the diffusion from paeonolloaded liposome in hydrogel was studied in vitro. Results: The results showed that the average particle size of paeonol-loaded liposome was about 401 nm, the potential was -17.8 mV, and the entrapment efficiency was above 45%. The viscosity of paeonol- loaded liposome in hydrogel was 23.972×10-3 Pa*s, and the diffusion rate from paeonol-loaded liposome in hydrogel in vitro was obviously slower than that from the other paeonol preparations. Conclusion: The conclusions could be drawn that paeonol-loaded liposome in hydrogel was a kind of novel preparation, and its diffusion in vitro had obvious controlled-release characteristics, which further proved that it might improve the bioavailability of paeonol.

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Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.4.6 ◽

2012 ◽

Vol 4 (4) ◽

pp. 1557-1562 ◽

Cited By ~ 1

Author(s):

Ankit Anand Kharia ◽

A K Singhai ◽

R Verma

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Average Particle Size ◽

Chlorinated Solvents ◽

Entrapment Efficiency ◽

The Body ◽

Hydrophilic Polymers ◽

Polydispersity Index ◽

Average Particle ◽

Loading Efficiency

The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.

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Formulation and Evaluation of Ketoprofen Using β-Cyclodextrin Capped Silver Nanoparticles

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.3.7 ◽

2021 ◽

Vol 14 (3) ◽

pp. 5501-5507

Author(s):

Kiranmai Mandava ◽

Kruthika Lalit ◽

Venu Madhav Katla

Keyword(s):

Particle Size ◽

Silver Nanoparticles ◽

Average Particle Size ◽

Amorphous State ◽

Entrapment Efficiency ◽

In Vitro Dissolution ◽

Average Particle ◽

Dissolution Studies ◽

Drug Entrapment Efficiency

The objective of the study was to develop silver nanoparticles loaded with Ketoprofen (Ag-KP) for increasing the drug solubility and thereby its bioavailability. Ag-KP were prepared by the solvent evaporation method using β-Cyclodextrin as a biodegradable polymer. Different formulations of Ag-KP were characterized for the drug entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), particle size analysis, X-ray diffraction studies (XRD), scanning electron microscopy (SEM) and in-vitro dissolution studies. The optimized formulation (F6) has shown an average particle size of 167.8 ± 3.46 nm,zeta potential of -23.7 ± 1.46 mV. FTIR revealed that the drug showed good excipient compatibility. XRD studies showed that the drug has changed from crystalline to amorphous state. In all formulations, F6 formulation (optimized) exhibited high drug entrapment efficiency (∼93%). SEM studies indicated the shape of Ag-KP was roughly spherical with smooth surface. In vitro dissolution studies showed that Ag-KP from F6 formulation was 94.3 ± 4.9% but for the marketed formulation, it is only 84.6 ± 3.7% in 12 hours and F6 was found to be found stable for three months at both refrigerated and room temperature (RT).

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Formulation and Evaluation of Nanosuspension Formulations of Ramipril using Hydrophilic Polymers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.1.5 ◽

2015 ◽

Vol 8 (1) ◽

pp. 2735-2741

Author(s):

Pankaj P Nerker ◽

Hitendra Mahajan ◽

Sagar Deore ◽

Pradyumn Ige

Keyword(s):

Particle Size ◽

Dissolution Rate ◽

Average Particle Size ◽

Entrapment Efficiency ◽

Hydrophilic Polymers ◽

In Vitro Dissolution ◽

Average Particle ◽

Antisolvent Precipitation ◽

Enhanced Dissolution

Nanosuspensions provide convenient formulations for improving the bioavailability and drug delivery. The objective of the investigation was to develop stable nanosuspension formulation of ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability. Ramipril is a potent antihypertensive drug, which act by inhibiting the angiotensin-converting enzyme. Nanosuspension was developed by antisolvent precipitation followed by high-pressure homogenization using hydrophilic polymers such as HPMC E5, HPMC E15, PVP K30, PVP K25, and PVA. The resulting nanosuspension was transformed into dry powder by freeze-drying process. Among all five formulations a formulation was choosen on the basis of results obtained from comparative study between different polymers based nanosuspension formulation of ramipril. The nanosuspension prepared was then evaluated for particle size, polydispesivity index, zeta potential, entrapment efficiency, saturated solubility study, scanning electron microscopy, differential scanning colorometry, and X ray diffraction. The combination of soya lecithin and pluronic F-68 as stabilizers yield nanosuspension with the smallest average particle size. The formulation of ramipril based on HPMC E 15 (Formulation B) shown enhanced dissolution rate. In which more than 60% of the drug was dissolved in the first 20 min compared to less than 25% of the pure drug within the same time period. The increase in the in vitro dissolution rate, nano size may favourably affect bioavailability.

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Preparation of Poly[lactic-co-glycolic] Acid Nanospheres and Its Role in Hepatoma Cells

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2021.18627 ◽

2021 ◽

Vol 21 (2) ◽

pp. 977-986

Author(s):

Zhongxing Shi ◽

Jinping Li ◽

Hongwei Liang ◽

Hongbo Hu ◽

Huijie Jiang

Keyword(s):

Particle Size ◽

Release Rate ◽

Hepg2 Cells ◽

Glycolic Acid ◽

Drug Loading ◽

Average Particle Size ◽

Plga Nanoparticles ◽

Toxin Gene ◽

Average Particle

Poly[lactic-co-glycolic] acid (PLGA) targeting nanoparticles AFP/PLGA/Dt386, loaded with Dt386 plasmid of diphtheria toxin gene, modified by Alpha fetoprotein (AFP) monoclonal antibody, is prepared. Its physical and chemical properties and its effect on HepG2 cells are studied. Firstly, Dt386 expression plasmid pET11a/Dt386 is constructed and PLGA nanoparticles are prepared by emulsion solvent evaporation (ESE). Scanning electron microscope (SEM) is used to observe its morphology. Laser Particle Sizer is used to measure the particle size. In addition, the encapsulation efficiency, drug loading and in vitro release rate of PLGA nanoparticles are measured. Carboxy fluorescein and rhodamine fluorescein are used to double label IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanospheres, respectively, the entry of nanospheres into HepG2 cells are observed at 3 h and 12 h. The effect of AFP/PLGA/Dt386 nanospheres on the migration of HepG2 cells is examined by wounding healing assay. Transwell chamber experiment is used to detect the effect of AFP/PLGA/Dt386 nanospheres on the invasion of HepG2 cells. MTT method is utilized to determine the inhibitory activity of nanoparticles on HepG2 cell proliferation. After treated with IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanoparticles for 48 hours, flow cytometry is used to detect the apoptosis rate and cell cycle of HepG2 cells in each group. The results show that the prepared nanospheres have regular morphology, flat surface, average particle size of 265.72±12.46 nm, zeta potential of −18.15 mV. The average entrapment efficiency and drug loading are 78.48±1.71% and 3.16±0.35%, respectively. The nanoparticles release slowly and stably in vitro. At the 10th day, the release rate reaches 75.13%. PLGA nanospheres can effectively protect DNA from nuclease degradation. The results show that AFP/PLGA/Dt386 nanospheres have biological targeting effect and can be enriched in cells. AFP/PLGA/Dt386 nanoparticles can significantly inhibit the migration, invasion and proliferation of HepG2 cells, and promote apoptosis.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i11.35670 ◽

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.

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Physical Evaluation of Transfersome that Contains Pandan Leaves Extract (Pandanus amaryllifolius R.)

Journal Of Tropical Pharmacy And Chemistry ◽

10.25026/jtpc.v5i4.307 ◽

2021 ◽

Vol 5 (4) ◽

pp. 369-374

Author(s):

Rini Ambarwati ◽

Yulianita Yulianita

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Average Particle Size ◽

Particle Morphology ◽

Entrapment Efficiency ◽

Average Particle ◽

Hard Tissue ◽

Long Time ◽

Original Size ◽

Active Substances

Pandan leaves have been researched and have effectiveness in the treatment of burns. The process of healing burns takes a long time and cause a hard tissue because it loses its elasticity, making it difficult to penetrate. In this study, pandanus leaves were formulated into the nanovesicle carrier system, namely trasfersom. Transfersomes have the ability to deform, namely the ability to reduce the particle size 5-10 times from the original size when passing through the gaps between cells so that transfersom can increase the penetration of active substances. The three formulas used are based on the ratio of concentrations of trasfersome vesicles, namely phospholipids and span 80. Formula 1 is (90:10), Formula 2 (85:15) and Formula 3 (80:20). The best formula is determined based on transfersom characterization, including particle size and PDI (solidispersity index), zeta potential, entrapment efficiency, deformability, and TEM particle morphology. The results showed that Formula 3 (80:20) is the most stable formula with an average particle size of 730.1 ± 4.9 nm, PDI value <0.7, zeta potential - 9.94 ± 1.02 mV, efficiency absorption 80.23%, and the deformability value 6.225.

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Preparation of progesterone nanoparticles and evaluation of its effect on the capacitation of Bovine spermatozoa used in the in Vitro Fertilization

International Journal of Drug Delivery ◽

10.5138/09750215.2224 ◽

2018 ◽

Vol 9 (4) ◽

pp. 125

Author(s):

Saber Abd-Allah ◽

Mai Ralan ◽

Hanaa Suliman ◽

Tamer Essam ◽

Heba F Salem

Keyword(s):

Average Particle Size ◽

Spherical Shape ◽

Aqueous Solubility ◽

Average Particle ◽

Sperm Capacitation ◽

Vitro Fertilization ◽

Transmission Electron ◽

Bovine Spermatozoa ◽

Sperm Functions

Progesterone (P) has been reported to affect several sperm functions especially capacitation and acrosome reaction. The main problem of (P) is its low aqueous solubility. So formulation of progesterone nanoparticles (PN) will enhance its solubility. This study was conducted to produce nanosized progesterone (NP) and assess its biocompatibility. Therefore, nine progesterone formulations were prepared and characterized. Data analysis revealed only one formula of P showed nanosized particle (1-100 nm) with an average particle size (95±5 nm), and spherical shape as seen by Transmission Electron Microscope(TEM). Motile spermatozoa were separated from frozen-thawed semen by a swim-up procedure and capacitated in IVF-TALP medium with NP or P or without treatments (control) and incubated for 3h at 38°C and evaluated every 1 hour (h) interval. Ovarian oocytes were matured and fertilized in vitro with frozen-thawed bull sperm capacitated in vitro with NP or P or control (without NP, P) and incubated at 39C in 5% CO2 incubator for 24h and then examined for evidence of fertilization. In conclusion, this study demonstrates that nanosized progesterone is highly efficient for sperm capacitation. In addition to the use of nanosized progesterone in sperm capacitation produces more fertilized oocytes than the progesterone after In Vitro Fertilization (IVF).

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