scholarly journals Preparation and physicochemical characterization of Eudragit® RL100 Nanosuspension with potential for Ocular Delivery of Sulfacetamide

2010 ◽  
Vol 13 (4) ◽  
pp. 510 ◽  
Author(s):  
Bivash Mandal ◽  
Kenneth S Alexander ◽  
Alan T Riga
Keyword(s):  
Zeta Potential ◽  
Bacterial Infections ◽  
Room Temperature ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Freeze Dried ◽  
Drug Entrapment Efficiency

Purpose: Polymeric nanosuspension was prepared from an inert polymer resin (Eudragit® RL100) with the aim of improving the availability of sulfacetamide at the intraocular level to combat bacterial infections. Methods: Nanosuspensions were prepared by the solvent displacement method using acetone and Pluronic® F108 solution. Drug to polymer ratio was selected as formulation variable. Characterization of the nanosupension was performed by measuring particle size, zeta potential, Fourier Transform infrared spectra (FTIR), Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), drug entrapment efficiency and in vitro release. In addition, freeze drying, redispersibility and short term stability study at room temperature and at 40C were performed. Results: Spherical, uniform particles (size below 500 nm) with positive zeta potential were obtained. No significant chemical interactions between drug and polymer were observed in the solid state characterization of the freeze dried nanosuspension (FDN). Drug entrapment efficiency of the selected batch was increased by changing the pH of the external phase and addition of polymethyl methacrylate in the formulation. The prepared nanosuspension exhibited good stability after storage at room temperature and at 40C. Sucrose and Mannitol were used as cryoprotectants and exhibited good water redispersibility of the FDN. Conclusion: The results indicate that the formulation of sulfacetamide in Eudragit® RL100 nanosuspension could be utilized as potential delivery system for treating ocular bacterial infections.

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

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

Characterization, Intestinal Absorption and Pharmacokinetics of Long-Circulating Nanoparticles Loaded with Panaxnotoginseng saponins

2013 ◽  
Vol 662 ◽  
pp. 227-232
Author(s):  
Guo Wei Zhao ◽  
Xu Long Chen ◽  
Xin Li Liang ◽  
Zheng Gen Liao ◽  
Chun Liu Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Oral Administration ◽  
Intestinal Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Male Rats ◽  
Scanning Calorimetry ◽  
Time Curve ◽  
Vitro Release

The aim of the present study was to increase bioavailability after oral administration. In this study, Panaxnotoginseng saponins (PNS) was entrapped within the long-circulating nanoparticles (LCNs) by the multiple emulsion method. The PNS-LCNs were characterized in terms of size, zeta potential, morphology, thermal properties, drug entrapment efficiency (EE), and in vitro release of the PNS. In addition, the intestinal absorption of PNS-LCNs in vitro was investigated. The pharmacokinetics of PNS-LCNs following oral administration was determined over 72 h in male rats. It was found that the mean particle size and zeta potential of the PNS-LCNs were 147±4.5nm and −44.7±1.5mV, respectively, and the entrapment efficiency (EE) was 53.93%±0.69%. differential scanning calorimetry (DSC) indicated that PNS has different states in PNS-LCNs and original PNS. The release pattern of the PNS-LCNs followed the Weibull model. The release parameters (T50, TD) were observed to be higher for PNS-LCNs compared with original PNS (p< 0.01) in vitro release. The intestinal absorption study indicated that the intestinal permeability coefficient (Papp) of PNS-LCNs was higher than original PNS’s. The pharmacokinetics of PNS-LCNs was studied after oral administration to male rats, PNS-LCNs provided greater area under the concentration-time curve (AUC), higher plasma concentration (Cmax), longer mean residence time (MRT) and median time to maximum drug concentration (Tmax). LCNs could be used for improving permeability and increased bioavailability after oral administration of PNS.

Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles

2021 ◽  
Vol 29 (9_suppl) ◽  
pp. S1555-S1568
Author(s):  
Vibha Chourasiya ◽  
Sarvesh Bohrey ◽  
Archna Pandey
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Amlodipine Besylate ◽  
Process Yield ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.

Preparation and Characterization of Freeze-dried Liposomes Loaded with Amphotericin B

2019 ◽  
Vol 14 (1) ◽  
pp. 65-73 ◽  
Author(s):  
Tran Thi Hai Yen ◽  
Le Nho Dan ◽  
Le Hoang Duc ◽  
Bui Thanh Tung ◽  
Pham Thi Minh Hue
Keyword(s):  
Amphotericin B ◽  
Freeze Drying ◽  
Entrapment Efficiency ◽  
Freezing Process ◽  
Scanning Calorimetry ◽  
Citrate Buffer ◽  
Lipid Film ◽  
Freeze Dried ◽  
Liposomal Suspension

Background: Amphotericin B (AmB) is a drug of choice in the therapy of systemic fungal infection because of its board-spectrum antifungal activity. However, its conventional formulation has many side effects such as acute and chronic nephrotoxicity. Liposomes have been developed to reduce the drug’s toxicity. However, they had to meet strict stability criteria. In general, liposomes can be freeze-dried to inhibit liposomes infusion, phospholipids degradation during storage. Liposomal size usually increases after freeze-drying because of being influenced by many factors in freezing, lyophilizing and rehydration processes. Therefore, cryoprotectants are used to stabilize liposomal vesicles during freeze-drying process. </P><P> Objective: In the present study, we developed AmB liposomal suspension and lyophilized liposomes loaded with AmB, evaluated the effect of different cryoprotectants on the characterization of freeze-dried AmB liposomes. </P><P> Methods: In this study, AmB liposomes were prepared from hydrogenated soy phosphatidylcholine, distearoylphosphatidylglycerol and cholesterol by thin lipid film hydration method using different hydrate mediums likely: Glucose solution, citrate buffer, phosphate buffer. High-pressure homogenization and extrusion methods were used to reducing vesicles size. Dynamic light scattering was used to characterize liposomal size, and size distribution. HPLC method was used to assay drug and determine entrapment efficiency. Liposomal suspension was lyophilized with different cryoprotectants: Sucrose, mannitol, lactose, trehalose and glycerol. Differential scanning calorimetry was used to study lyophilized cake. </P><P> Results: We found that liposomal suspension with hydration medium10 mM citrate buffer pH 5.5 had a small average size (<100nm) and narrow distribution (PDI <0.2). Sucrose and trehalose stabilized vesicles size during freezing process, and lyophilized liposomes with sucrose and trehalose had an elegant appearance, yellow, compact cake. DSC study showed that sucrose and trehalose in lyophilized cake were amorphous. The cake was rehydrated within 10 seconds to form liposomal suspension, in which vesicles size was less than 140 nm. </P><P> Conclusion: We have developed successfully AmB liposomal suspension and lyophilized liposomes loaded with AmB. Sucrose and trehalose can be used as cryoprotectants in the freeze-drying and reconstitution process.

Nifedipine-Loaded Polymeric Nanocapsules: Validation of a Stability-Indicating HPLC Method to Evaluate the Drug Entrapment Efficiency and In Vitro Release Profiles

2013 ◽  
Vol 96 (2) ◽  
pp. 276-281 ◽  
Author(s):  
Andréa Granada ◽  
Monika Piazzon Tagliari ◽  
Valdir Soldi ◽  
Marcos Antônio Segatto Silva ◽  
Betina Ghiel Zanetti-Ramos ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Hplc Method ◽  
Stability Indicating ◽  
Polymeric Nanocapsules ◽  
Drug Entrapment Efficiency ◽  
High Entrapment Efficiency

Abstract A simple stability-indicating analytical method was developed and validated to quantify nifedipine in polymeric nanocapsule suspensions; an in vitro drug release study was then carried out. The analysis was performed using an RP C18 column, UV-Vis detection at 262 nm, and methanol–water (70 + 30, v/v) mobile phase at a flow rate of 1.2 mL/min. The method was validated in terms of specificity, linearity and range, LOQ, accuracy, precision, and robustness. The results obtained were within the acceptable ranges. The nanocapsules, made of poly(ε-caprolactone), were prepared by the solvent displacement technique and showed high entrapment efficiency. The entrapment efficiency was 97.6 and 98.2% for the nifedipine-loaded polymeric nanocapsules prepared from polyvinyl alcohol (PVA) and Pluronic F68 (PF68), respectively. The particle size and zeta potential of nanocapsules were found to be influenced by the nature of the stabilizer used. The mean diameter and zeta potential for nanocapsules with PVA and PF68 were 290.9 and 179.9 nm, and –17.7 mV and –32.7 mV, respectively. The two formulations prepared showed a drug release of up to 70% over 4 days. This behavior indicates the viability of this drug delivery system for use as a controlled-release system.

Introducing Electrospray as a Potent Technique to Deliver Chitosan/pDNA Nanoparticles to Eukaryotic Cells

2021 ◽  
Vol 66 ◽  
pp. 73-84
Author(s):  
Farzaneh Saeedi Landi ◽  
Babak Negahdari ◽  
Fariba Esmaeili ◽  
Sedigheh Kolivand ◽  
Amir Amani
Keyword(s):  
Zeta Potential ◽  
Transfection Efficiency ◽  
Low Cost ◽  
Gene Transfection ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Ratio Size ◽  
Agarose Electrophoresis ◽  
One Step

Electrospray technique has received increasing attentions for intracellular gene delivery as well as production of nanoparticles. In this study, chitosan/pDNA nanoparticles with N/P ratio of 5 were prepared and transferred to HEK293T cells by electrospray technique. Physicochemical characterization of prepared nanoparticles, including size, zeta potential and entrapment efficiency was performed and attachment of pDNA to chitosan was confirmed by gel agarose electrophoresis. Moreover, transfection efficiency was investigated using flow cytometry. MTT assay was performed for cell viability studies. Nanoparticles were prepared at three pDNA concentrations of 10, 55 and 100 μg/ml in fixed N/P ratio. Size of nanoparticles was obtained as 110, 188 and 240 nm, using DLS. SEM showed size of 102.34 ± 10.66 nm for samples having 55 μg/ml pDNA. Zeta potential and entrapment efficiency were +25 mv and 85±4%m respectively. The effect of pDNA concentration, electrospray time and incubation time on transfection efficiency was investigated using Box-Behnken design. Percent of GFP-positive cells was 41.05 ± 3.04% which was taken as an indicator of transfection efficiency. Transfection efficiency of this method was then compared with that of calcium phosphate (31.1 ± 2.4%), showing improved efficiency. Considering the fact that electrospray is an easy, low cost, one-step process which makes low damage to cells and produces monodispersed nanoparticles, the method is introduced as a fascinating approach in gene transfection.

Development of lipid nanocarriers for tuberculosis treatment: evaluation of suitable excipients and nanocarriers

2021 ◽  
Vol 18 ◽  
Author(s):  
Gabriela Hädrich ◽  
Cristiana Lima Dora ◽  
Gustavo Richter Vaz ◽  
Raphael Boschero ◽  
Arthur Sperry Appel ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Delivery Systems ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Lipid Nanocarriers ◽  
Low Toxicity

Background: Lipid nanocarriers have been widely tested as drug delivery systems to treat diseases due to their bioavailability, controlled release, and low toxicity. For the pulmonary route, the Food and Drug Administration favors the use of substances generally recognized as safe, as well as biodegradable and biocompatible to minimize the possibility of toxicity. Tuberculosis (TB) remains a public health threat worldwide, mainly due to the long treatment duration and adverse effects. Therefore, new drug delivery systems to treat TB are needed. Objective: Physicochemical characterization of different lipid-based nanocarriers was used to optimize carrier properties. Optimized systems were incubated with Mycobacterium tuberculosis to assess whether lipid-based systems act as an energy source for the bacteria, which could be counterproductive to therapy. Method: Several excipients and surfactants were evaluated to prepare different types of nanocarriers using high-pressure homogenization. Results: A mixture of trimyristin with castor oil was chosen as the lipid matrix after differential scanning calorimetry analysis. A mixture of egg lecithin and PEG-660 stearate was selected as an optimal surfactant system as this mixture formed the most stable formulations. Three types of lipid nanocarriers, solid lipid nanoparticles, nanostructured lipid carriers (NLC), and Nano emulsions, were prepared, with the NLC systems showing the most suitable properties for further evaluation. It may provide the advantages of increasing the entrapment efficiency, drug release, and the ability to be lyophilized, producing powder for pulmonary administration being an alternative to entrap poor water-soluble molecules. Conclusion: Furthermore, the NLC system can be considered for use as a platform for the treatment of TB by the pulmonary route.

Moxifloxacin Loaded Polymeric Nanoparticles for Sustained Ocular Drug Delivery

2012 ◽  
Vol 5 (2) ◽  
pp. 1727-1734
Author(s):  
A P Gadad ◽  
Sharath Chandra P ◽  
Dandagi P M ◽  
V S Mastiholimath
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Glycolic Acid ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Eye Drops ◽  
Potential Drug ◽  
Sustained Effect ◽  
Drug Entrapment Efficiency

Efficient drug delivery to the ocular region is a challenging goal. Only a very small amount (about l-3%) of the dosage actually penetrates through the cornea and reaches intraocular tissues. To overcome these problems of conventional dosage forms, novel drug delivery systems like nanoparticles were designed. Moxifloxacin-loaded poly (lactic-co-glycolic acid) nanosuspension was prepared with the aim of providing sustained effect for ocular delivery for 24 hours. Nanosuspensions were prepared by nanoprecipitation method using poly(lactic-co-glycolic acid) and evaluated for particle size, surface morphology, zeta potential, drug entrapment efficiency, in vitro release and ex vivo transcorneal permeability, and were compared with marketed products. Microbiological efficacy was tested against Staphylococcus aureus and Pseudomonas aeroginosa using cup plate method. Spherical uniform particles (202.5 nm) with a polydispersity index of 0.226 and negative zeta potential (– 25.45 mV) were obtained for MF4 (drug to polymer ratio 1:0.4). Drug entrapment efficiency for MF4 was found to be 83.1%. The cumulative percent drug release for formulation MF4 after 24 hours was 86.1%, showing a sustained effect in controlling the bacterial conjunctivitis thereby avoiding frequent administration of dosage. MFX-loaded PLGA nanoparticles (MF4) showed a significantly higher drug permeation capability compared to the commercial marketed eye drops in ex vivo transcorneal permeation studies and also showed better antimicrobial efficacy compared to the marketed formulation. The results indicate that Moxifloxacin-loaded PLGA nanosuspension could be utilized as a potential drug delivery system for sustained release in ophthalmic application.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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