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 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 OPTIMIZATION AND CHARACTERIZATION OF DOXORUBICIN LOADED SOLID LIPID NANOSUSPENSION FOR NOSE TO BRAIN DELIVERY USING DESIGN EXPERT SOFTWARE

2021 ◽  
pp. 45-57
Author(s):  
VIRAG A. SHAH ◽  
JAYVADAN K. PATEL
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
High Speed ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
Solid Lipid ◽  
Stirring Time

Objective: The goal of the current study was to investigate the possible use of solid lipid nanosuspension (SLNs) as a drug delivery method to boost doxorubicin (DOX) brain-targeting performance after intranasal (i. n.) administration.  Methods: 33 factorial design was applied for optimization by using lipid concentration, surfactant concentration, and High-speed homogenizer (HSH) stirring time as dependent variables, and their effect was observed on particles size, Polydispersity index (PDI), and entrapment efficiency.  Results: With the composition of Compritol® 888 ATO (4.6 % w/v), tween 80 (1.9 % w/v), and HSH stirring time, the optimized formula DOX-SLNs prepared (10 min). Particle size, PDI, zeta potential, entrapment efficiency, percent in vitro release were found to be 167.47±6.09 nm, 0.23±0.02, 24.1 mV, 75.3±2.79, and 89.35±3.27 percent in 24 h, respectively, for optimized formulation (V-O). No major changes in particle size, zeta potential, and entrapping efficiency were found in the stability studies at 4±2 °C (refrigerator) and 25±2 °C/60±5% RH up to 3 mo.  Conclusion: Following the non-invasive nose-to-brain drug delivery, which is a promising therapeutic strategy, the positive findings confirmed the current optimized DOX-loaded SLNs formulation.

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 PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES

2017 ◽  
Vol 10 (3) ◽  
pp. 103 ◽  
Author(s):  
Megha Sharma ◽  
Seema Kohli ◽  
Abhisek Pal
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Appreciable Amount ◽  
Average Particle

ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.

Indinavir-Loaded Nanostructured Lipid Carriers to Brain Drug Delivery: Optimization, Characterization and Neuropharmacokinetic Evaluation

2019 ◽  
Vol 16 (4) ◽  
pp. 341-354 ◽  
Author(s):  
Mohammad Nasiri ◽  
Amir Azadi ◽  
Mohammad Reza Saghatchi Zanjani ◽  
Mehrdad Hamidi
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Free Drug ◽  
Average Particle ◽  
The Brain

Purpose: As an anti-retroviral Protease Inhibitor (PI), Indinavir (IDV) is part of the regimen known as Highly Active Anti-Retroviral Therapy (HAART) widely used for Human Immunodeficiency Virus (HIV) infection. The drug efficiency in treatment of the brain manifestations of HIV is, however, limited which is mainly due to the efflux by P-glycoprotein (P-gp) expressed at the Blood-Brain Barrier (BBB). Methods: To overcome the BBB obstacle, NLCs were used in this study as carriers for IDV, which were optimized through two steps: a “one-factor-at-a-time” screening followed by a systematic multiobjective optimization. Spherical smooth-surfaced Nanoparticles (NPs), average particle size of 161.02±4.8 nm, Poly-Dispersity Index (PDI) of 0.293±0.07, zeta potential of -40.62±2.21 mV, entrapment efficiency of 93±1.58%, and loading capacity of 9.15±0.15% were obtained after optimization which were, collectively, appropriate in terms of the objective of this study. Result: The surface of the optimized NPs was, then, modified with human Transferrin (TR) to improve the drug delivery. The particle size, zeta potential, and PDI of the TR-modified NLCs were 185.29±6.7nm, -28.68±3.37 mV, and 0.247±0.06, respectively. The in vitro release of IDV molecules from the NPs was best fitted to the Weibull model indicating hybrid diffusion/erosion behavior. Conclusion: As the major in vivo findings, compared to the free drug, the NLCs and TR-NLCs displayed significantly higher and augmented concentrations in the brain. In this case, NLC and TR-NLC were 6.5- and 32.75-fold in their values of the brain uptake clearance compared to free drug.

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

Drug Research ◽  
2020 ◽  
Author(s):  
Sonia Pahuja ◽  
Shweta Aggarwal ◽  
Prerna Sarup
Keyword(s):  
Average Particle Size ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Average Particle ◽  
Chitosan Microspheres ◽  
Optimum Parameters ◽  
Sustained Effect

Abstract Objective The present investigation entailed determination of effect of diverse cross-linking agents on Losartan Potassium loaded chitosan microspheres. The emulsion cross-linking method was employed to formulate the microspheres with an endeavour to achieve maximum sustained effect. Methods The FTIR studies revealed absence of any interaction between Losartan and chitosan. The emulsion cross linking method was accomplished in three steps encompassing formation of an aqueous and oily phase, emulsification and cross-linking. A total of eighteen Losartan formulations were developed using six different cross-linkers at three varying level were screened for optimum parameters. The in vitro drug release parameters of optimum formulations (LC3, LE3, LF3, LG3, LS3 and LV3) containing citric acid, epichlorohydrin, formaldehyde, glutaraldehyde, suphuric acid and vanillin as cross-linkers were assessed to determine the sustained effect. Results The values of evaluated parameters including percent yield (94.67%), average particle size (51.19 µm), drug content (44.38 mg) and entrapment efficiency (88.77%) connoted LG3 as the best formulation. Additionally, the values of relative measure of skewness (β1=0.01 and γ1=0.10) and platykurtic (β2=1.26) size distribution were least for LG3 with spherical shape and smooth surface as revealed by SEM studies. Conclusion The outcome of in vitro release and other characterizations of microspheres explicitly revealed glutaraldehyde as the best cross-linker amongst the cross-linkers used herewith. The maximum sustained effect (lasting over a period of 24 h) accompanied with higher MDT and t50% with lower%DE and Q14h values thus corroborated the objective of attaining sustained release of Losartan.

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 Preparation and characterization of domperidone nanoparticles for dissolution improvement

2018 ◽  
Vol 27 (1) ◽  
pp. 39-52
Author(s):  
Mohammed Sabar Al-lami ◽  
Malath H. Oudah ◽  
Firas A. Rahi
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Precipitation Method ◽  
Average Particle ◽  
Antisolvent Precipitation ◽  
Stirring Time

This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formula was obtained with lowest average particle size of 84.05. This formula was studied for compatibility by FTIR and DSC, surface morphology by FESEM and crystalline state by XRPD. Then domperidone nanoparticles were formulated into a simple capsule dosage form in order to study of the in vitro release of drug from nanoparticles in comparison raw drug and mixture of polymer:drug ratios of 2:1. The release of domperidone from best formula was highly improved with a significant (p? 0.05) increase.

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

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.

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