Formulation and Evaluation of Polymeric Nanoparticle by Nano-Precipitation Method (original) (raw)
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Formulation and evaluation of acyclovir nanosuspension for enhancement of oral bioavailability
Asian Journal of Pharmaceutics, 2014
A cyclovir, an antiviral drug used against herpes simplex virus and varicella zoster virus. The dose ranges between 200 and 800 mg and the oral bioavailability is 10-20%, which decreases as the dose is increased. The aim of this research work was to formulate and characterize nanosuspensions of acyclovir with an intention to increase the oral bioavailability. Nanosuspensions were prepared by the precipitation-ultra sonication method and the effects of important process parameters i.e., precipitation temperature, stirring speed, end point temperature of probe sonicator, energy input and sonication time were investigated systematically, the optimal nanosuspension (particle size 274 nm) was obtained at values of 4°C, 10,000 rpm, 30°C, 600 Watt and 20 min, respectively. The nanosuspension was lyophilized using different matrix formers and sucrose (100% w/w to drug) was found to prevent agglomeration and particle size upon reconstitution was found to be 353 nm. The lyophilized nanocrystals appeared flaky in scanning electron microscopy images, the X-ray powder diffraction and differential scanning calorimetry analysis showed the nanoparticles to be in the crystalline state. Ex vivo permeation study for calculating absorption rate and in vivo bioavailability area under the curve both showed threefold increase over marketed suspension.
Objective of present work was to formulate polymeric microparticles of acyclovir using β-cyclodextrin by solvent evaporation method and kneading technique. Four different ratios were fabricated in each case. Sodium lauryl sulfate (4%) was utilized as intestinal permeation enhancer in this study. Prepared microparticles were characterized for micromeritic properties i.e., angle of repose, Hausnerís ratio, Carrís index, bulk density and tapped density, entrapment efficiency, zeta size and zeta potential, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder x-ray diffraction, scanning electron microscopy, transmission electron microscopy, optical microscopy and permeability studies across chicken intestine. Kinetic mod- els: zero order, first order, Higuchi and Korsmeyer Peppas were applied on release data. Based upon the results of entrapment efficiency (81.25% and 74.50%), product yield (92.50% and 85.50%), permeability (85.18% and 82.05%), x-ray diffraction (amorphous nature), and solubility etc., (1 : 2) drug-polymer ratio was declared the best. Moreover, solid dispersions (1 : 2) had shown promising results. A new potential approach for solubility, bioavailability and permeability enhancement of acyclovir and other BCS class IV drugs was successfully established.
Pakistan journal of pharmaceutical sciences, 2019
Objective of the study was to perform a physico-chemical modification of low molecular weight chitosan (CTS) followed by its use in the formulation of nanoparticles carrier of Acyclovir (ACY). Modified polymer was used to develop ACY loaded nanoparticles in order to achieve optimal response and to minimize toxic effects of ACY. CTS were dissolved in varying concentrations of potassium hydroxide solution to synthesize N, O-carboxymethylated chitosan (N,O-CMC). Synthesized derivative was further processed with different concentrations of TPP (0.3%, 0.5% and 1%) and ACY to prepare nanoparticles. N,O-CMC and prepared formulations were characterized by Fourier transform infrared spectroscopy (FTIR). Furthermore, scanning electron microscopy (SEM) was done to observe the surface morphology, zeta size and zeta potential for particle size analysis, in vitro dissolution to find out the release pattern and kinetic modeling was done to observe the release mechanism and pattern of the drug. Res...
Formulation and physicochemical characterization of chitosan/Acyclovir co-crystals
Pharmaceutical Development and Technology, 2013
In the current study, the influence of chitosan on the dissolution rate and bioavailability of acyclovir has been illustrated through the preparation of co-crystals by simple solvent change method. Chitosan was precipitated on acyclovir crystals using sodium citrate as the salting out agent. The pure drug and the prepared co-crystals using different concentrations and molecular weights of chitosan were characterized in terms of drug content, particle size, thermal behavior, IR analysis, surface morphology, in vitro drug release and physical stability. The results obtained showed that the practical yield of the prepared co-crystals was found to be inversely proportional to chitosan concentration. The drug content of the co-crystals was uniform among the different batches. The prepared co-crystals showed a slower drug release when compared to that of pure drug. The considerable change in the dissolution rate of acyclovir from optimized crystal formulation was attributed to the wetting effect of chitosan, the reduction in drug crystallinity and the altered surface morphology. The thermograms showed a decrease in the melting enthalpy of acyclovir indicating a disorder in the crystalline content whereas IR spectroscopy studies revealed an interaction between acyclovir and chitosan. The optimized co-crystals were stable for three months at 40°C and 75 ± 5% RH.
Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles
American Journal of Advanced Drug Delivery, 2016
Acyclovir sodium is an antiviral drug used to treat herpes, chicken pox and herpes skin infections. Acyclovir sodium potential as an antiviral drug is limited by its low oral bioavailability (20-30%) with short half-life (2-3 hours) with poor plasma protein binding. There is an opportunity to utilize Acyclovir sodium as an antiviral drug by enhancing the bioavailability by formulation technology. In this paper solid microparticle (o/w) of Acyclovir was prepared by melt dispersion technique. The characterization of drug using scanning electron microscopy, FT-IR, particle size, percentage yield, drug loading capacity, hausner's ratio and carr's index, bulk density and tapped density. In vitro drug release studies using phosphate buffer has shown as formulation F5 sustained release for 17 hrs.
Colloids and Surfaces B: Biointerfaces, 2020
This study investigated the feasibility of polysaccharide-coated poly(n-butyl cyanoacrylate) (PBCA) nanoparticles for oral delivery of acyclovir (ACV). PBCA nanoparticles were obtained by the emulsion polymerization method. Chitosan was chemically modified to obtain N,N,N-trimethylchitosan (TMC), which was used to coat the nanoparticles (PBCA-TMC). Nanoparticles were characterized by dynamic light scattering, zeta potential, differential scanning calorimetry (DSC), atomic force microscopy (AFM), cytotoxicity, and the effect on the transepithelial electrical resistance (TEER) of the Caco-2 cells. The size of the coated nanoparticles (296.2 nm) was significantly larger than uncoated (175.0 nm). Furthermore, PBCA nanoparticles had a negative charge (-11.7 mV), which was inverted to highly positive values (+36.5 mV) after coating. DSC analysis suggested the occurrence of the coating, which was confirmed by AFM images. The MTT assay revealed concentrationdependent cytotoxicity for the core-shell nanoparticles. Additionally, PBCA-TMC caused a significant but reversible decrease in the Caco-2 cell monolayer TEER. Entrapped ACV (PBCA-ACV-TMC), a Biopharmaceutical Classification System class III drug substance, increased approximately 3.25 times the Papp of ACV in the Caco-2 permeability assay. The nanoparticles were also able to provide in vitro ACV controlled release using media with different pH values (1.2; 6.8; 7.4). Accordingly, this new core-shell nanoparticle showed the potential to improve the oral delivery of ACV.
Colloids and Surfaces B: Biointerfaces, 2010
Acyclovir (ACV)-Eudragit (EUD) nanoparticles (NPs) were prepared using both EUD RS 100 and RL 100 with different charge density. The effect of charge intensity on particle size, encapsulation efficiency, and in vitro dissolution was assessed. The bioavailability of ACV NP colloids were evaluated in human volunteers, compared with commercial product using a validated LC-MS/MS method with a lower limit of quantification (LLOQ) of 0.02 g/ml. EUD RL 100 with higher ammonium groups gave smaller NPs than EUD RS 100. The surface charge of the polymer did not affect encapsulation efficiency and in vitro dissolution. In human volunteers, both F2 and F5 colloidal nanosuspensions prepared with EUD RS and RL respectively in drug to polymer ratio 1:3 sustained the oral absorption of ACV, expressed by the significant lower C max , significant delayed T max and the significant higher HVD t 50%Cmax . The mean C max of F2, F5, and Zovirax ® were 0.61 ± 0.06, 0.73 ± 0.07 and 0.92 ± 0.21 g/ml respectively. Furthermore, the AUC 0-12 of F2 and F5 was significantly higher than that of Zovirax ® with values of 4.37 ± 0.88, 5.14 ± 0.87 and 3.21 ± 0.53 g/ml h respectively. The higher AUC 0-12 for both F2 and F5 reflected high relative bioavailability of 136.2% and 159.9% respectively compared to commercial ACV tablets.
Pharmaceutics, 2018
Acyclovir is not a good candidate for passive permeation since its polarity and solubility limit is partitioning into the stratum corneum. This work aims to develop a new topical formulation for the acyclovir delivery. New chitosan nanospheres (NS) were prepared by a modified nano-emulsion template method. Chitosan NS were characterized by Dynamic Light Scattering (DLS), Transmission Electron Microscopy (TEM), and an in vitro release study. The in vitro skin permeation experiment was carried out using Franz cells and was equipped with porcine skin. Biological studies were performed on the Vero cell line infected by HSV-1 and HSV-2 strains. The acyclovir loaded chitosan NS appeared with a spherical shape, a size of about 200 nm, and a negative zeta potential of about 40.0 mV. The loading capacity of the drug was about 8.5%. In vitro release demonstrated that the percentage of acyclovir delivered from the nanospheres was approximately 30% after six hours. The in vitro skin permeation ...
International Journal of Applied Pharmaceutics, 2022
Objective: Acyclovir is widely used as a potent antiviral drug to treat viral infections of herpes and varicella-zoster families. Unfortunately, the drug has a very poor oral bioavailability character (15-30%). The purpose of this study was to develop a formulation of acyclovir suspension with a simple suspension method using Na-CMC (carboxymethylcellulose sodium), and to carry out quality control of the finished product. Methods: The formulation was developed by designing variations in Na-CMC concentration and quality control, including pH, viscosity, dispersibility, storage stability, microscopic measurement, sedimentation volume, and evaluation of acyclovir levels. Quality control is to evaluate the suspension in order to obtain good and stable physicochemical properties of the suspension. Results: Design variations of Na-CMC concentrations of 1.4%, 1.5%, and 1.6% resulted in a homogeneous suspension and easily dispersed perfectly. The three formulas did not have a significant difference in the value of viscosity, permeability, and sedimentation volume, which were not significant. All formulas have pseudoplastic flow properties, with good particle size uniformity in the range of 0-13 µm. The stability of pH during storage time was shown by the formula with 1.5% Na-CMC. Conclusion: The acyclovir suspension with 1.5% Na-CMC concentration was the best compared to the other formulas in terms of stability and physicochemical properties.