scholarly journals SYNTHESIS AND STABILITY OF RESVERATROL-CONJUGATED GOLD NANOPARTICLES MODIFIED WITH POLYETHYLENE GLYCOL

2020 ◽  
pp. 230-236
Author(s):  
RADITYA ISWANDANA ◽  
RICHA NURSELVIANA ◽  
SUTRIYO SUTRIYO
Keyword(s):  
Particle Size ◽  
Gold Nanoparticles ◽  
Polyethylene Glycol ◽  
Zeta Potential ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Test Results ◽  
Novel Method ◽  
The Stability ◽  
Phosphate Buffered Saline

Objective: Gold nanoparticles (AuNPs) are highly useful for drug delivery, but their application is limited by their stability as they readily aggregate.This issue can be prevented by adding a stabilizing agent such as resveratrol (RSV), which is a polyphenol derived from plants, that is used to preventcancer. Therefore, we propose a novel method to prepare stable RSV-conjugated nanoparticles modified with polyethylene glycol (RSV-AuNP-PEG).Methods: In the first step, the Turkevich method was used to synthesize the AuNPs. Then, PEG was added as stabilizer agent and conjugated with RSV.The synthesized conjugates were characterized using ultraviolet-visible spectrophotometry, Fourier transform infrared spectroscopy, particle sizeanalysis, and high-performance liquid chromatography.Results: The obtained RSV-AuNP-PEG had a particle size of 83.93 nm with a polydispersity index (PDI) of 0.562 and formed a translucent purple-redfluid in solution. The zeta potential was −22.9 mV, and the highest entrapment efficiency was 75.86±0.66%. For comparison, the RSV-AuNP solutionwas purple and turbid, the particle size was 51.97 nm with a PDI of 0.694, and the zeta potential was −24.6 mV. The stability test results showed thatthe storage stability of RSV-AuNP-PEG was better than that of AuNP-RSV. Further, the RSV-AuNP-PEG was shown to be most stable in 2% bovine serumalbumin (BSA) while the AuNP-RSV was most stable in 2% BSA in phosphate-buffered saline pH 7.4.Conclusion: These results show that modification of RSV-conjugated AuNPs with PEG effectively prevents their aggregation in storage, but only incertain mediums.

scholarly journals EFFECT OF TRANSFERSOME ON THE STABILITY AND ANTIOXIDANT ACTIVITY OF GLUTATHIONE IN ANTIAGING CREAMS

2020 ◽  
pp. 149-155
Author(s):  
HARMITA HARMITA ◽  
ISKANDARSYAH ◽  
FRIAINI ZAHRA MURTI
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
Phase Separation ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Antioxidant Compound ◽  
Ic50 Value ◽  
The Stability ◽  
Franz Diffusion Cells

Objective: Glutathione is an important antioxidant compound that is added to various cosmetic preparations. This study compared the stability,antioxidant activity, and penetration of glutathione creams formulated with and without transfersome, a commonly used carrier system.Methods: The particle size of the transfersome was 55.65 nm, with a polydispersity index of 0.398 and an entrapment efficiency of 66.22%. Duringcycling and centrifugal testing, the creams (with and without transfersome) did not change color or demonstrate phase separation. Chemical stabilityanalyses of the products were performed using high-performance liquid chromatography.Results: The remaining glutathione content in the transfersome cream was 83.44%, while that of the non-transfersome cream was 47.92%. In thepenetration test using Franz diffusion cells, the transfersome cream demonstrated a cumulative penetration of 4474.44 μg/cm2, with a cumulativeconcentration percentage of 39.60% and a flux of 510.38 μg/cm−2h−1. In contrast, the non-transfersome cream demonstrated a cumulative penetrationamount of 2793.80 μg/cm2, with a cumulative concentration percentage of 24.73% and a flux of 340.12 μg/cm−2h−1. In addition, the IC50 value of thetransfersome cream preparation was 11.89 μg/mL, while that of the non-transfersome preparation was 15.57 μg/mL.Conclusion: Our findings indicate that the use of transfersome increases the stability and penetration of glutathione in cream preparations.

scholarly journals FORMULATION AND OPTIMIZATION OF NIFEDIPINE LOADED NANOCARRIERS

2021 ◽  
pp. 311-317
Author(s):  
ASHWINI JADHAV ◽  
BINOY VARGHESE CHERIYAN
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Physicochemical Characteristics ◽  
Good Choice ◽  
The Stability

Objective: The main aim of this study to formulate a nifedipine-loaded nanocarrier for improving solubility and bioavailability. Methods: To improve the solubility of drug, nifedipine-loaded nanocarrier (lipotomes) were prepared by using the film lipid hydration technique. lipotomes were prepared by using tween 80, which is used for increasing solubility and cetyl alcohol for lipophilic environment. Drug excipients interaction determined by FTIR. lipotomes were characterized for particle size, Entrapment efficiency and zeta potential. lipotomes were optimized by using Design-Expert 12 software. Optimized formula further lyophilized by using different cyroproyectant to improve the stability and oral administration of the drug. Results: FTIR shows there was no interaction between formulation ingredients. Mean particle size, entrapment efficiency, zeta potential was determined and found to be 308.1 nm, 96.7%, 20.1mV, respectively. Surface morphology of lipotomes was observed by a scanning electron microscope (SEM). Optimized lipotomes was lyophilized with Mannitol (8% w/v) was the ideal cryoprotectant to retain the physicochemical characteristics of the OLT formulation after lyophilization. Conclusion: Nifedipine loaded nanocarrier was successfully prepared, using film hydration method. Which have good particle size, EE% and zeta potential. After lyophilization no significant changes was observed in particle size with good physical stability, so it could be a good choice for conventional drug delivery system by doing further investigation as in vitro and in vivo study

scholarly journals Andrographolide-loaded ethosomal gel for transdermal application: Formulation and in vitro penetration study

2021 ◽  
Author(s):  
Nooryza Martihandini ◽  
Silvia Surini ◽  
Anton Bahtiar
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Weight Ratio ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Transmission Electron Micrograph ◽  
C 30 ◽  
The Stability

Background: Andrographolide is a phytoconstituent with anti-inflammatory activity, however, the compound’s poor oral bioavailability has hindered its effective formulation for oral administration. This study, therefore, aims to develop an ethosome for improving andrographolide penetration through the transdermal delivery system. Methods: This study developed 3 ethosome formulas with different andrographolide-phospholipid weight ratios (1:8, 1:9; 1:10), using the thin-layer dispersion-sonication method. Subsequently, the ethosomes were evaluated for particle size, polydispersity index, zeta potential, morphology, as well as entrapment efficiency, and incorporated into a gel dosage form. Subsequently, an in vitro penetration study was performed using Franz diffusion cells for 24 hours and the stability of the gels at 5 ± 2°C, 30 ± 2°C, and 40 ± 2°C, were studied for 3 months. Results: The results showed the optimal formula was E2, a 1:9 weight ratio formula of andrographolide and phospholipid. Based on the transmission electron micrograph, E2 possessed unilamellar, as well as spherical-shaped vesicles, and exhibited superior characteristics for transdermal delivery, with a particle size of 89.95 ± 0.75 nm, polydispersity index of 0.254 ± 0.020, a zeta potential of -39.3 ± 0.82 mV, and entrapment efficiency of 97.89 ± 0.02%. Furthermore, the cumulative andrographolide penetration and transdermal flux for the ethosomal gel of E2 (EG2) were 129.25 ± 4.66 µg/cm2 and 5.16 ± 0.10 µg/cm2/hours, respectively. All the ethosomal gel formulations exhibited improved penetration enhancement of andrographolide, compared to the nonethosomal formulations. Also, the andrographolide levels in the ethosomal and nonethosomal gels after 3 months ranged from 98.13 to 104.19%, 97.93 to 104.01%, and 97.23 to 102.26% at storage temperatures of 5 ± 2°C, 30 ± 2°C/RH 65% ± 5%, and 40 ± 2°C/RH 75% ± 5%, respectively. Conclusions: This study concluded that encapsulation into ethosome enhances andrographolide delivery through the skin.

scholarly journals SYNTHESIS AND STABILITY OF RESVERATROL-GOLD NANOPARTICLE-POLYETHYLENE GLYCOL-FOLIC ACID CONJUGATES

2020 ◽  
pp. 237-241
Author(s):  
SUTRIYO SUTRIYO ◽  
RADITYA ISWANDANA ◽  
FIRDA MARETHA IVARIANI
Keyword(s):  
Particle Size ◽  
Folic Acid ◽  
Polyethylene Glycol ◽  
Zeta Potential ◽  
High Surface ◽  
Average Particle Size ◽  
Average Particle ◽  
Nanoparticle Stability ◽  
Model Drug ◽  
The Stability

Objective: Gold nanoparticles (AuNPs) can be used as targeted drug delivery systems, however, AuNPs have high surface energy and easily aggregate,thus negatively impacting nanoparticle stability. Therefore, it is necessary to add a stabilizing agent to AuNPs. To synthesize AuNPs stabilized bypolyethylene glycol conjugated to folic acid (FA), thus creating a model drug (resveratrol [RSV]) carrier that targets FA receptors on cancer cells.Methods: AuNPs were synthesized using the Turkevich method and stabilized by adding FA conjugated to polyethylene glycol (PEG). After RSV wasloaded, the conjugate was physically characterized and subjected to stability tests.Results: The RSV-AuNP had an average particle size of 51.97 nm (polydispersity index [PDI] 0.694, zeta potential – 24.6 mV). The RSV-AuNP-PEG-FAconjugate (RSV-AuNP-PEG-FA) had an average particle size of 195.6 nm (PDI=0.233, zeta potential=−21.1 mV). Stability tests showed that RSV-AuNPPEG-FA was more stable than RSV-AuNP. Furthermore, RSV-AuNP-PEG-FA and RSV-AuNP were more stable in buffer pH 7.4 and bovine serum albumin2% than in buffer pH 4, cysteine 1%, and NaCl 0.9% solutions.Conclusion: PEG-FA conjugates can improve the stability of RSV-loaded AuNP.

Novel Simultaneous Identification of Capsaicin and It’s Quantification in Transferosome Formulation By HP-TLC Technique

2020 ◽  
Vol 17 (1) ◽  
pp. 172-183
Author(s):  
Nandanwadkar Shrikrishna Madhukar Hema ◽  
Mastiholimath Vinayak Shivamurthy ◽  
Pulija Karunakar
Keyword(s):  
Particle Size ◽  
Quality Control ◽  
Regression Analysis ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Average Recovery ◽  
Morphological Studies ◽  
Drug Entrapment Efficiency ◽  
Different Levels

Introduction: Capsaicin (8-methy-N-vanillyl-6-nonenamide), a potential analgesic derived from Capsicum annuum (Chili peppers), widely used from ancient times for its pharmacological activities such as anti-inflammatory, anti-oxidant and analgesic and provides relief from migraine and diabetes. But for obvious reasons, capsaicin cannot be administered directly. The present work was designed with a focus to comply with mandatory requirement in various pharmacopeias to know the actual content of API present in final formulations. The formulation (TS3) consisting of 3% lipid, with 4:6 ratio of the polymer and solvent, was found to be the optimized formulation, which gave the best evaluation with regard to the particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies and highest drug entrapment efficiency (68.34±4.24)%. The prepared transferosome formulation was subjected to characterization by validated HP-TLC method consisting of N-Hexane: Tert- Iso-butyl-methyl ether in ratio (5:15) v/v. Linearity was performed in the range of 50-1500 ng/spot with LOD/LOQ 50 ng and 150 ng, with regression analysis (R) of 99.91%. Recovery analysis was performed at 3 different levels at 80, 100 and 120 with an average recovery of 106.97%, respectively. Till now, no analytical method has been reported, associated with the characterization of pharmaceutical nano-forms (Capsaicin), like transferosomes. Thus, the maiden validated HP-TLC method for concurrent analysis of capsaicin as API in nano-transferosome may be employed in process quality control of formulations containing the said API. Background: The irritability and adverse effects post application, leading to inflammation and neural pain at the site of administration of newly Capsaicin API and its chemical entities and marketed formulations are usually related to poor permeability, leading to drug complex reactions in the development phases or therapeutic failure along with the quantification of the same in blood plasma. However, advancement in drug formulations with the use of polymer: alcohol ratio and modernized analytical techniques for the quantification of Pharmaceutical APIs seems to be emerging and promising for overcoming pain and related inflammatory complications by formulating the APIs in Transferosome formulation with Validated HP-TLC technique being used as an effective economic and precise tool for quantitative analysis of APIs in their respective nano-forms. Objective: The study proposes a novel standardized method development and validation of pharmaceutical nanoforms with Capsaicin as API. Method: Capsaicin Transferosomes were formulated using Ultra probe sonication by utilizing different proportions of phospholipid 90G dissolved in a mixture of ethanol and propylene glycol. The formulation was subjected to Dynamic Light Scattering (DLS) technique for nano-particle analysis followed by characterization with respect to particle size, polydispersity index, zeta potential and entrapment efficiency. The morphological study of vesicles was determined using SEM and TEM. A Validated HP-TLC method for the identification and determination of Capsaicin in transferosomes formulation was performed as per the ICH guidelines. Results: The formulation gave the best evaluation for particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies (SEM & TEM) and highest drug entrapment efficiency (68.34±4.24)%. DSC thermograms and FTIR spectral patterns confirmed no physical interaction by polymers with API. The prepared formulation was then characterized using HP-TLC method. The best resolution was found in NHexane: Tert-Isobutyl methyl ether in a ratio of 5:15 v/v. The Rf was found to be 0.3±0.03. Linearity was performed in a range of 50-1500 ng/spot, with regression analysis (R) of 99.91% Further, recovery analysis was done at 3 different levels as 80, 100 and 120 with an average recovery of 106.97%. The LOD/LOQ was found to be 50 and 150 ng, respectively. Precision was carried out in which % RSD was found to be precise and accurate. Conclusion: The outcomes of the present study suggested that the proposed novel formulation analyzed by Validated planar chromatographic technique (HP-TLC) for Capsaicin quantification in nanoforms may be employed as a routine quality control method for the said API in various other formulations.

scholarly journals FORMULATION AND CHARACTERIZATION OF TIMOLOL MALEATE-LOADED NANOPARTICLES GEL BY IONIC GELATION METHOD USING CHITOSAN AND SODIUM ALGINATE

2019 ◽  
pp. 48-54 ◽  
Author(s):  
RISA AHDYANI ◽  
LARAS NOVITASARI ◽  
RONNY MARTIEN
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Ionic Gelation ◽  
Timolol Maleate ◽  
Optimum Formula

Objective: The objectives of this study were to formulate and characterize nanoparticles gel of timolol maleate (TM) by ionic gelation method using chitosan (CS) and sodium alginate (SA). Methods: Optimization was carried out by factorial design using Design Expert®10.0.1 software to obtain the concentration of CS, SA, and calcium chloride (CaCl2) to produce the optimum formula of TM nanoparticles. The optimum formula was characterized for particle size, polydispersity index, entrapment efficiency, Zeta potential, and molecular structure. Hydroxy Propyl Methyl Cellulose (HPMC) K15 was incorporated into optimum formula to form nanoparticles gel of TM and carried out in vivo release study using the Franz Diffusion Cell. Results: TM nanoparticles was successfully prepared with concentration of CS, SA, and CaCl2 of 0.01 % (w/v), 0.1 % (w/v), and 0.25 % (w/v), respectively. The particle size, polydispersity index, entrapment efficiency, and Zeta potential were found to be 200.47±4.20 nm, 0.27±0.0154, 35.23±4.55 %, and-5.68±1.80 mV, respectively. The result of FTIR spectra indicated TM-loaded in the nanoparticles system. In vitro release profile of TM-loaded nanoparticles gel showed controlled release and the Korsmeyer-Peppas model was found to be the best fit for drug release kinetics. Conclusion: TM-loaded CS/SA nanoparticles gel was successfully prepared and could be considered as a promising candidate for controlled TM delivery of infantile hemangioma treatment.

scholarly journals Ex-vivo Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model

2019 ◽  
Vol 28 (2) ◽  
pp. 37-45
Author(s):  
Haithem N Abed ◽  
Ahmed A. Hussein
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Oral Absorption ◽  
Ex Vivo ◽  
Dabigatran Etexilate ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carrier ◽  
Loading Capacity ◽  
Intestinal Permeation

Abstract The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of  92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal permeation study using the non-everted sac model shows four folds increment in the permeation of DE-NLCs compared to dabigatran etexilate suspension (DE-S).

scholarly journals Effect of Potato Pulp Pectic Polysaccharide on the Stability of Acidified Milk Drinks

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5632
Author(s):  
Weixuan Sun ◽  
Wenhan Yang ◽  
Yuxue Zheng ◽  
Huiling Zhang ◽  
Haitian Fang ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Neutral Sugar ◽  
Lower Serum ◽  
Pectic Polysaccharide ◽  
Potato Pulp ◽  
Lower Viscosity ◽  
Stabilizing Effect ◽  
New Ideas ◽  
The Stability

In order to broaden the application of potato pulp pectic polysaccharide (PPP) in stabilizing acidified milk drinks (AMDs) and investigate the stabilizing effect and physical properties of AMDs prepared with PPP, a comparative study was made among PPP, commercial high methoxyl pectin (HMP) and low methoxyl pectin (LMP). The zeta potential, rheology, particle size and serum separation of AMDs were evaluated after preparing with PPP, HMP and LMP, respectively. Results indicated that PPP led to lower serum separation than LMP (14.65% for AMDs prepared with 0.5% PPP compared to 25.05% for AMDs prepared with 0.5% LMP), but still higher than HMP (9.09% for AMDs prepared with 0.5% HMP). However, narrower particle size distribution and lower viscosity of AMDs was achieved by PPP than by LMP and HMP. PPP can electrostatically adsorb on the surface of casein and its abundant neutral sugar side chains would provide steric hindrance to prevent casein flocculation in AMDs. Our results might provide some new ideas for the application of PPP in improving the stability of AMDs.

scholarly journals FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 10 (12) ◽  
pp. 14 ◽  
Author(s):  
M. Yasmin Begum ◽  
Prathyusha Reddy Gudipati
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Size Analysis ◽  
Compatibility Study ◽  
Solid Lipid ◽  
Poly Dispersity Index

Objective: The aim of present work was to formulate and evaluate Dasatinib (DST) loaded solid lipid nanoparticles (SLNs) as a potential anticancer drug delivery system by enhancing its solubility.Methods: SLNs consist of a solid lipid matrix where the drug was incorporated. Surfactants of GRAS grade were used to avoid aggregation and to stabilize the SLNs. DST-SLNs formulations of varying concentrations were prepared by high speed homogenization technique and evaluated for drug excipients compatibility study, poly-dispersity index, particle size analysis, surface morphology, zeta potential and drug release features.Results: It was observed that DST-SLNs with optimum quantities of poloxomer: lecithin ratio showed 88.06% drug release in 6h with good entrapment efficiency of 76.9±0.84 %. Particle size, Poly dispersity index, zeta potential and drug entrapment efficiency for the optimized formulation was found to be optimum. Stability studies revealed that the entrapment efficiency of the SLN dispersion stored in 4 °C was stable.Conclusion: Thus, it can be concluded that formulations of DST loaded SLNs are suitable carriers for improving the solubility and dissolution related problems. 

scholarly journals Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 197 ◽  
Author(s):  
Doaa Hassan ◽  
Rehab Abdelmonem ◽  
Menna Abdellatif
Keyword(s):  
Particle Size ◽  
Intraocular Pressure ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Duration Of Action ◽  
Corneal Permeability ◽  
Glaucoma Treatment

This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.

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