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

2019 ◽  
pp. 188-193 ◽  
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.

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

Coatings ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 439 ◽  
Author(s):  
Hibah M. Aldawsari ◽  
Nabil A. Alhakamy ◽  
Rayees Padder ◽  
Mohammad Husain ◽  
Shadab Md
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Plga Nanoparticles ◽  
Steady Increase ◽  
Average Particle

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.

scholarly journals FORMULATION AND OPTIMIZATION AND IN VITRO CHARACTERIZATION OF OLANZAPINE LIPOSOME

2021 ◽  
pp. 109-114
Author(s):  
G. NETHRA VANI ◽  
M. ALAGUSUNDARAM ◽  
K. B. CHANDRASEKAR
Keyword(s):  
Zeta Potential ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Prediction Method ◽  
Entrapment Efficiency ◽  
Zero Order ◽  
Nasal Delivery ◽  
Brain Targeting ◽  
Average Particle

Objective: Olanzapine (OZ) is a thioeno benzodiazepine class second-generation or atypical antipsychotic that selectively binds to central dopamine D2 and serotonin (5-HT2c) receptors used for the treatment of schizophrenia and bipolar disorder. The present paper is aimed at developing an optimized liposome-loaded OZ as an approach for brain targeting through the nasal route for effective therapeutic management of schizophrenia. Methods: The OZ liposomes were prepared by the thin-film hydration method. Various independent variable such as phospholipid, cholesterol and sonication time was optimized by using Design-Expert® Software to obtain the dependent variables of entrapment efficiency, vesicle size and zeta potential. The optimized formulation was predicted based on the response obtained by the point prediction method. Results: The entrapment efficiency of the formulation was range between 72.9 and 85.1 %. The average particle size of all the 15 experimental runs lies between the minimum and maximum values of the size 258.33 to 325.32 nm, respectively. The zeta potential ranges from-27.53 to-11.46 mV. The optimized formulation for characterized for its morphology by Transmission Electron Microscopy (TEM). In vitro release studies of OZ-loaded liposomal formulation was carried by dialysis sac method using pH 7.4 phosphate buffer (PBS) as a medium. The maximum release was found to be 98.43±1.2 % up to 24 h. The R2 zero-order kinetics and Korsmeyer-Peppas model was found to be 0.9919 and 0.9664, respectively. The zero-order shows the best-fit model with a highest R2 value exhibiting better correlation and the ‘n’ value was also found to be 0.85; indicating both diffusion-controlled and swelling-controlled drug release that is anomalous transport. Conclusion: The results, clearly states that the prepared formulations justify the parameters and OZ might be a suitable candidate to target the brain through nasal delivery.

scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Interaction ◽  
Precipitation Method ◽  
Pharmacokinetic Studies ◽  
Average Particle

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

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

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.

scholarly journals FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE

2019 ◽  
pp. 438-446
Author(s):  
GOWTHAMI B ◽  
NIHITHA S ◽  
SANTHI PRIYA NAGAM ◽  
RAMA RAO NADENDLA
Keyword(s):  
Fluidized Bed ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Lag Phase ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Coating Technique ◽  
Fluidized Bed Coating

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers. Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer). Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics. Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design.

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

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.

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

2012 ◽  
Vol 4 (4) ◽  
pp. 1557-1562 ◽  
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.  

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

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).

GASTRORETENTIVE MICROBALLOONS OF RIBOFLAVIN: FORMULATION AND EVALUATION

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (04) ◽  
pp. 47-52
Author(s):  
S. C. B Penjuri ◽  
R. Nagaraju ◽  
S. Shaik ◽  
S. Damineni ◽  
S. R. Poreddy ◽  
...  
Keyword(s):  
Drug Release ◽  
Average Particle Size ◽  
Proximal Part ◽  
Diffusion Method ◽  
Average Particle ◽  
Dsc Studies ◽  
Enhanced Absorption ◽  
Percentage Yield ◽  
Emulsion Solvent Diffusion Method

Gastroretentive dosage forms are useful to extend release of drugs having a narrow window of absorption in the upper intestine and for drugs degraded by higher pH or for drugs with local action in the proximal part of the GI tract. In the present study, an attempt was made to prepare microballoons of riboflavin by emulsion solvent diffusion method by using HPMC and ethylcellulose in order to extend the drug release in the upper GIT, which may result in enhanced absorption and thereby improved bioavailability. The size and surface morphology of riboflavin microballoons were characterized by optical and scanning electron microscopy. FTIR and DSC studies revealed no drug excipient interaction. Average particle size of microballoons was found to be between 126.8±2.26 to 163.4±2.52 μm. Microballoons were found to be spherical in shape with smooth surface texture. Percentage yield of the microballoons was satisfactory. In vitro buoyancy of the optimized riboflavin microballoons was found to be 96.24±0.08%, indicating good floating in stomach. Cumulative amount of drug release from microballoons at the end of 12 hr was 99.78±2.78 % and followed Highuchi diffusion kinetics and super case II transport.

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