Docetaxel-Loaded Chitosan-Cholesterol Conjugate-Based Self-Assembled Nanoparticles for Overcoming Multidrug Resistance in Cancer Cells

Cholesteryl hemisuccinate (CHS)-conjugated chitosan (CS)-based self-assembled nanoparticles (NPs) were developed for enhancing the intracellular uptake of docetaxel in multidrug resistance (MDR)-acquired cancer cells. CHS-CS was successfully synthesized and self-aggregation, particle size, zeta potential, drug entrapment efficiency, and in vitro drug release of docetaxel-loaded CHS-CS NPs were tested. The optimized NPs had a mean hydrodynamic diameter of 303 nm, positive zeta potential of 21.3 mV, and spherical shape. The in vitro release of docetaxel from the optimized CHS-CS NPs in different pH medium (pH 6.0 and 7.4) revealed that the release was improved in a more acidic condition (pH 6.0), representing a tumor cell’s environment. The superior MDR-overcoming effect of docetaxel-loaded CHS-CS NPs, compared with docetaxel solution, was verified in anti-proliferation and cellular accumulation studies in MDR-acquired KBV20C cells. Thus, CHS-CS NPs could be potentially used for overcoming the MDR effect in anticancer drug delivery.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s4.31721 ◽

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..

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Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

Current Drug Delivery ◽

10.2174/1567201817666200902150646 ◽

2020 ◽

Vol 17 ◽

Author(s):

Bhaskar Kurangi ◽

Sunil Jalalpure ◽

Satveer Jagwani

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Topical Application ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

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

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i5.27564 ◽

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.

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

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2021v13i5.41137 ◽

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.

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Formulation and evaluation of albendazole nanoparticle

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i1-s.2239 ◽

2019 ◽

Vol 9 (1-s) ◽

pp. 16-22

Author(s):

Yerikala Ramesh ◽

Koorapati Balasaradhi ◽

Kaki Rohan Abhilash

Keyword(s):

In Vitro Release ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Homogenization Method ◽

Drug Molecules ◽

Sustained Effect ◽

Drastic Increase ◽

Size Of Particles ◽

Novel Drug

Therefore, there is a need to develop alternative novel drug delivery formulations of albendazole to improve its intestinal absorption and also to reduce its side effects during regular therapy. The Albendazole nanoparticles were prepared by hot homogenization method under high magnetic stirring using stearic acid as lipid and poloxamer 188 was used as surfactant. Initial pre-formulation studies using FTIR spectroscopy reveals that there are no interactions between Albendazole and other excipients and hence they can be used for the preparation of nanoparticles. The entrapment efficiencies varied from a minimum of 43.56 ± 0.95 % to a maximum of 85.1 ±0.58% and it can be concluded that higher amount of lipid is necessary for obtaining a good entrapment efficiency. The drug content of albendazole nanoparticles for all formulation ranges from 65.8% to 98.1%. A spherical shape was observed for the particles and the particles had a smooth morphology when examined under SEM. In vitro release studies of the formulations carried out in pH 7.4 PBS showed that the total amount of drug is released for 9hrs with sustained effect. That the formulations showed a drastic increase in size when stored at room temperature where the size of particles increased from an initial to 343.7 ±7.9 nm at the end of 1 month to 898.1 ± 5.8 nm at the end of 2 months. Entrapment efficiency of the formulation was determined at each interval to ensure that the drug molecules didn’t undergo any degradation during storage. Keywords: Albendazole, Nanoparticles, Particle size, Entrapment efficiency.

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DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2019v11i7.33115 ◽

2019 ◽

pp. 109-115

Author(s):

AHMED GARDOUH ◽

Samar H. Faheim ◽

Samar M. Solyman

Keyword(s):

Zeta Potential ◽

Release Kinetics ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Homogenization Method ◽

Nanostructured Lipid Carriers ◽

Scanning Calorimetry ◽

Release Study ◽

Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

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STUDY OF ENHANCED ANTI-INFLAMMATORY POTENTIAL OF NIGELLA SATIVA IN TOPICAL NANOFORMULATION

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i7.22966 ◽

2018 ◽

Vol 10 (7) ◽

pp. 41 ◽

Cited By ~ 3

Author(s):

Faisal Obaid Alotaibi ◽

Gulam Mustafa ◽

Alka Ahuja

Keyword(s):

Zeta Potential ◽

Size Distribution ◽

Therapeutic Potential ◽

Ex Vivo ◽

Nigella Sativa ◽

In Vitro Release ◽

Spherical Shape ◽

Active Constituent ◽

Anti Inflammatory

Objective: Formulate a nanocarrier for enhancing the anti-inflammatory activity of thymoquinone (Tq), a major active constituent of Nigella sativa.Methods: Nanoformulation of Tq was developed by low energy emulsification techniques. NanoTqs were pre-screened by different thermodynamic stability tests, followed by in vitro release, zeta potential, viscosity, the transmittance (%), globule size distribution and ex vivo studies. The morphology of the optimized NanoTq was determined by transmission electron microscopy (TEM) which revealed fairly spherical shape and good correlation with particle size distribution study. The formulation used for assessment of the anti-inflammatory potential and permeability enhancement contained mixture of essential oil of Nigella sativa: Capryol 90 (3:7, 10%, v/v), Tween 80 (21.75%, v/v), PEG 400 (7.25%, v/v) and double distilled water (61%, v/v).Results: The in vitro permeation of Tq from optimized formulations was found extremely significant (p<0.001) in comparison to apiTq. The steady state flux (Jss), the permeability coefficient (Kp) and enhancement ratio (Er) of NanoTq gel was determined and compared with apiTq. The comparative anti-inflammatory effects of the optimized formulations NanoTq, apiTq and DicloGel was assessed on the edema in the carrageenan-induced paw model in Wistar rats. Therapeutic potential of NanoTq was found statistically extremely significant (P<0.0001) compared to apiTq and insignificant comparable with standard DicloGel. Storage stability of NanoTq showed insignificant changes in the zeta potential, droplet size and was free from any physical instability.Conclusion: The optimized nano formulation with a lower dose of Tq showed better anti-inflammatory effects, indicating greater absorption capability through the stratum corneum.

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FORMULATION AND OPTIMIZATION OF ITRACONAZOLE PRONIOSOMES USING BOX BEHNKEN DESIGN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i2.23382 ◽

2018 ◽

Vol 10 (2) ◽

pp. 41

Author(s):

Ahmed M. Samy ◽

Afaf A. Ramadan ◽

Amal S.m. Abu El-enin ◽

Yasmin I. M. Mortagi

Keyword(s):

Zeta Potential ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Slow Phase ◽

Optimum Level ◽

Box Behnken Design ◽

Vesicle Size ◽

Transmission Electron ◽

Span 60

Objective: The aim of the present study was to obtain an optimized formula of itraconazole (ITC) proniosomes using Box Behnken design.Methods: Itraconazole proniosomes were prepared using span 60 and/or brij 35 as surfactants, cholesterol and lecithin as a penetration enhancer by slurry method. Various trials have been carried out for investigation of proniosomes. Parameters such as entrapment efficiency (EE%), in vitro drug release, zeta potential, vesicle size and Transmission Electron Microscope were assessed for evaluation of proniosomes.Results: Entrapment efficiency (EE%) was found to be between 78.56% and 95.46%. The release profile of itraconazole proniosomes occurred in two distinct phases, an initial phase for about 8 h, followed by a slow phase for 16 h. The release pattern shown by these formulations was Higuchi diffusion controlled mechanism. The zeta potential values for all itraconazole proniosomes were in the range of-21.71 to-34.53 mV which confirms their stability. All itraconazoleproniosomes formula was found to be nano-sized and were appeared to be spherical in shape with sharp boundaries. One way analysis of variance (ANOVA) study showed that HLB (X1) had the main effects on most responses (Y).Conclusion: Box behnken design facilitates optimization of the formulation ingredients on entrapment efficiency, in vitro release of itraconazole proniosomes, zeta potential and vesicle size. Finally, an optimum level of factors was provided by the optimization process.

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

Coatings ◽

10.3390/coatings10050439 ◽

2020 ◽

Vol 10 (5) ◽

pp. 439 ◽

Cited By ~ 3

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.

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USE OF LACTIC ACID AND SPAN 80 IN THE FORMULATION OF LIPID BASED IMIQUIMOD VESICLES FOR GENITAL WARTS

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15915 ◽

2017 ◽

Vol 9 (2) ◽

pp. 292

Author(s):

Saroj Jain ◽

Anupama Diwan ◽

Satish Sardana

Keyword(s):

Particle Size ◽

Lactic Acid ◽

Zeta Potential ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Genital Warts ◽

Formulation Development ◽

Span 80

Objective: The objective of present study was formulation development of imiquimod using lactic acid and span 80 for topical delivery to cure genital warts.Methods: Lipid based vesicles (LBV) of 2% imiquimod were prepared with phospholipoin 90G, ethanol, lactic acid and span 80 using central composite design. The prepared vesicles were optimized statistically and characterized for particle size, zeta potential, percentage entrapment efficiency (% EE) and transmission electron microscopy (TEM). The optimized LBV were incorporated into gel formulation which was evaluated and compared with control gel and marketed formulation.Results: The optimized vesicles had particle size 394.8±9.6 nm, zeta potential-16.5±2.5 mV, % EE 88.27±0.45 and TEM study confirmed the formation of vesicular structure with spherical shape. The gel formulation of imiquimod vesicles showed positive results like spreadability 14.3±0.34 gcm/s, viscosity 13500±1.67 cp, consistency 6.1±0.14 mm and extrudability 16.47±0.11 g/cm2. In vitro permeation amount of drug was remarkably lower (10.13 %) than control (87.17 %) and marketed formulation (27.46 %). Results of retained drug for both in vitro as well as in vivo permeation study and local accumulation efficiency (4.021±0.2292) were considerably higher for LBV gel than control (0.1008±0.002513) and marketed formulation (0.8314±0.0300). To understand the mechanism of interaction between skin and vesicles, fourier transform infra-red spectroscopy studies were also done. Results of skin irritancy test and histological examination revealed biocompatible nature of formulation.Conclusion: Results of in vitro and in vivo studies indicated that this vesicle gel formulation provided efficient and site specific dermal delivery of imiquimod for cure of genital warts.

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