scholarly journals BIODEGRADABLE LIPOSOMES FOR ACYCLOVIR-GOLD NANOPARTICLES AS AN EFFICIENT CARRIERFOR ENHANCED TOPICAL DELIVERY

Author(s):  
Heba F. Salem ◽  
Sabry M. Tamam ◽  
Sahar M. Lotayef

Objective: Gold nanoparticles and nanoliposomes are effective new technology in delivering the bioactive agents and enhancing their performance by increasing the bioavailability. The goal of the present study was the formulation of liposome for the use as a carrier for nanogold conjugated with acyclovir (ACV), an antiviral drug, to enhance ACV delivery.Methods: The gold nanoparticles were used as a capping agent for ACV and sodium citrate was used as reducing agent for the gold. Transmission electron microscopy was used for characterization and to study the morphological and structural properties of drug-metallic nanostructures. Nanoliposomes were formulated using different molar ratios of a positive charge inducer (stearyl amine) or a negative charge inducer (diacetyl phosphate), lecithin, cholesterol and Span 60.Results: Gold nanoparticles with a particle size of 10–20 nm were formed. This small size of the formed particles has a clear effect in reducing the gold nanoparticles toxicity and enhancing the cellular uptake. The amount of sodium citrate used in this preparation influences the size of the gold nanoparticle. The present study employed 1% trisodium citrate that contains a carboxylic group and this carboxylic group works as a reducing and capping agent to synthesize ACV-gold nanoparticles conjugate. Liposomal formula F6 had the highest entrapment efficiency approaching 42%, the low particle size of 160 nm, and zeta potential of 43.5 mV.Conclusion: It is evident from the study that the liposomes can be used as a carrier of ACV conjugated with gold nanoparticles. This new strategy could be used successfully in the treatment of viral infection.

Author(s):  
RADITYA ISWANDANA ◽  
RICHA NURSELVIANA ◽  
SUTRIYO SUTRIYO

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.


2013 ◽  
Vol 795 ◽  
pp. 726-731 ◽  
Author(s):  
Khatijah A. Yaacob ◽  
Gooi Wyn Gyn

The gold nanoparticles film has been successfully formed on the silicon wafer by self-assembled method. The gold colliods were prepared by chemical reduction method where sodium citrate (act as the reducing, capping and stabilizing agent) were added into the boiling 50ml of 0.01% tetrachloroauria acid (HAuCl4) solution in reflux system. Different particle size of gold colloids (AuNPs_1 and AuNPs_2) were produced by altering the amount of sodium citrate. The as-prepared gold colloids were characterized by UV - Vis spectrometry, Malvern particle size analyzer, zeta potential and XRD. Self-assembled method of Au nanoparticles were first start with the cleaning of silicon wafers using standard RCA cleaning, and followed by the piranha treatment to producing an OH-terminated surface. Then, the wafers were functionalized with organosilane molecule by immersing the silicon wafer in 10mM of surfactant in methanolic solution to produce self-assemble monolayers (SAMs) on silicon wafer surface. These layers were used to immobilize the gold nanoparticles from as-prepared gold colloid and result of the gold nanoparticles film on silicon wafer. Effect of surfactant ((3-aminopropyl) trimethoxysilane (APTMS) and (3-mercaptopropyl) trimethoxysilane (MPTMS)), effect of particle size of gold colloid (AuNPs_1 and AuNPs_2) and the effect of deposition time (0.5, 1.0, 1.5 and 2 hours) to the surface morphology such as surface coverage, inter-particle distance were studied in this work. The surface morphology of gold nanoparticles films were characterized by FESEM and AFM.


2013 ◽  
Vol 872 ◽  
pp. 94-105
Author(s):  
Mayra C. Ramirez-Camacho ◽  
Inga Tuzovskaya ◽  
Nina Bogdanchikova ◽  
Alexey Pestryakov ◽  
Arturo Susarrey-Arce ◽  
...  

Au nanoparticles (NPs) functionalized with L-cysteine (Cys) and cysteine-glycine (Cys-Gly) were synthetized. The AuNPs were prepared using sodium citrate as reducing agent. The influence of the molar concentrations of Cys and Cys-Gly, as well as the sodium citrate is studied on particle size and particle size distribution. TEM measurements revealed the formation of AuNPs with diameter in the range 5-35 nm which corresponds to nontoxic sizes [we should add a reference here, perhaps number one]. The optimal particle size for biomedical application along with narrow particle size distribution was observed for samples prepared with molar ratio of CAu:Ccitrate = 1:10. The results of UV-Vis spectroscopy revealed the interaction of the AuNPs with Cys and Gly-Cys demonstrated by a visible change in the absorption intensities of the plasmon peak located at 520 nm after AuNP functionalization and a slight shifting of this gold nanoparticles plasmon peak. Thus, any dielectric shell on surface of particles with more refraction index (and, correspondingly, dielectric function) can produce the particles with the red shift. Such effect of the surface shell with red-shift in the range of few nanometers observed for the AuNPs functionalized with Cys and Cys-Gly (Fig. 4) can be interpreted as thin or discontinuous layer of aminoacid molecules according to the data of optical spectra simulation.


2017 ◽  
Vol 901 ◽  
pp. 32-36
Author(s):  
Agustina Sus Andreani ◽  
Suyanta ◽  
Eko Sri Kunarti ◽  
Sri Juari Santosa

Gold nanoparticles (AuNPs) have been synthesised from adsorbed Au on hydrotalcite (Mg/Al HT-AA-Au) using SDS (sodium dodecyl sulfate) and sodium citrate as capping agent. Then, the nanoparticles were recovered into pure gold by centrifugation. It is shown that sodium citrate has better activity compared to SDS as the capping agent. The electronic spectra of the resulted AuNPs showed that the optimum pH, sodium citrate concentration and time of sonication were 5, 70 mM, and 2 h, respectively. The results showed that the average size of AuNPs was 32 nm at SPR 531 nm. By centrifugation at 13000 rpm for 8 min, gold dust of Au(0) can be obtained from the gold nanoparticles capped sodium citrate. Based on infrared spectra and XRD, it is proven that the gold dust still contains citric and Mg/Al HT.


2021 ◽  
Vol 11 (5) ◽  
pp. 110-114
Author(s):  
Harshita Jain ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar

The guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules put downing triumphant market until date, being commercially accessible in a variety of dosage forms for oral, topical and parenteral administrations. Clinical purpose of this drug is better to new antiviral agents due to its potential values such as suppression of recurrence, security profile, negligible drug interactions and being inexpensive. ACV is slightly water soluble, less permeable and poorly bioavailable, yet further potential antiviral molecule, the physicochemical alterations and new dosage form approaches resulted with more than 100 research efforts within a decade. The current study endeavored at the formulation of chitosan microspheres loaded with ACV to conquer the poor bioavailability and recurrent dose administration. Chitosan microspheres were prepared by emulsification technique by glutaraldehyde cross-linking. A variety of formulation and process variables such as polymer, glutaraldehyde, drug, span 80 concentrations, effect of stirring speed and stirring time were optimized. Formulated microspheres were characterized for its drug loading, invitro drug release, entrapment efficiency, surface morphology (SEM), particle size analysis and FTIR spectroscopy. The characterization of the fabricated microspheres demonstrated smooth surface with thin particle size allocation and entrapment efficiency of 80.8% for stirring speed batch. The prepared microspheres showed a controlled drug release of 93.2% over a period of 8 hrs with initial burst release of 56.7 % in the first 2hrs. The FTIR showed that there was no possible drug interaction among the drug and polymer. From the data’s obtained it can be concluded that the chitosan microspheres could be believed as a possible carrier for controlled drug delivery of ACV. Keywords: Acyclovir, Antiviral drug, Microspheres, Chitosan, Glutaraldehyde.


2020 ◽  
Vol 10 (3) ◽  
pp. 271-279
Author(s):  
Tran Thi Hai Yen ◽  
Nguyen Tran Linh ◽  
Vu Thi Thu Giang ◽  
Hoang Lan Anh

Objectives: Acyclovir (ACV) is an antiviral drug, which requires frequent dosing regimen because of poor oral bioavailability and short half-life. In this study, ACV nanoparticles were formulated using ammonium methacrylates copolymers such as Eudragit RS 100 (Eud RS) and Eudragit RL 100 (Eud RL) to prolong release drug, and increase bioavailability. Methods: ACV loaded nanoparticles were prepared by the solvent replacement technique and then were characterized by particle size, distribution, entrapment efficiency, differential scanning calorimeter, transmission electron microscope, and in-vitro drug release. Results: It was found that as drug:polymer ratio changed from 1:2 to1:5, particle size and drug entrapment efficiency increased significantly. ACV– Eud RS loaded nanoparticles had a larger mean diameter of 363 nm in comparison to 200 nm of ACV- Eud RL nanoparticles. DSC results showed that in the prepared ACV-Eud RS nanoparticles, the drug was presented in the amorphous phase and may have been molecularly dispersed in the polymer matrix, but in the ACV-Eud RL nanoparticles, the drug was presented in the particles and homogeneously dispersed in the polymeric matrix. The entrapment efficiency of AVC-Eud RS nanoparticles was higher than that of ACV-Eud RL nanoparticles. In vitro drug release study showed that the ratios of released drug from ACV-Eud RS nanoparticles in the range from 58±3.8 to 62.9±4.6%, which was lower than those from ACV-Eud RL nanoparticles, in the range from 73.3±4.9 to 77.9±2.9%. The release was found to follow the Weibull model with a Fickian diffusion mechanism for both ACVEud RS and ACV- Eud RL nanoparticles. Conclusion: These results suggest that ACV nanoparticles based on Eud RS100 and Eud RL100 could prolong the release of the drug.


Author(s):  
Ihsan K. Jasim ◽  
Shaimaa N. Abd Alhammid ◽  
Alaa A. Abdulrasool

  CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl. 5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM and AFM showed crystalline and porous nature of the nanosponges. The in vitro drug release study of the selected formula 5-FUNS2 exhibited the fastest dissolution rate which is 56% in the first hr. Different molar ratios of (cyclodextrin to crosslinker) (CD: DPC) has a proficient effect on complexation efficiency (CE), apparent stability constant (Kst) and entrapment efficiency of 5-FU. 5-FUNS2 with (1:4) molar ratio showed the best result of CE, Kst and entrapment efficiency. 5-FUNS2 gave a higher release rate than the 5-FU-BCD inclusion complex and 5-FU solution. Surface morphology of the prepared nanosponges by SEM, AFM indicate that nanosized and highly porous nanosponges was obtained. The overall results suggest that cyclodextrin nanosponges could be a promising 5-FU delivery system utilizing the suitable formula.


Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai

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.


Author(s):  
V K Verma ◽  
Ram A

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 


Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis


Sign in / Sign up

Export Citation Format

Share Document