Influence of the preparation method on the physicochemical properties of econazole-loaded poly(butyl cyanoacrylate) colloidal nanoparticles (original) (raw)
Related papers
Colloid and Polymer Science, 2010
Classically, drug-loaded poly(alkylcyanoacrylate) colloidal carriers are prepared by the drug entrapment during emulsion polymerization. However, a number of chemically sensitive drugs are unstable in the conditions of polymerization or can be irreversibly inactivated by the highly reactive monomer. Furthermore, the particle size distribution and the molecular weight of formed polymer depend strongly on the polymerization conditions. Here, we investigate the nanoprecipitation approach for the preparation of pure and drug-load poly(butylcyanoacrylate) nanoparticles. This method allows the successful entrapment of lipophilic and chemically labile drugs by avoiding the contact with highly reactive monomers. The anticancer agent chlorambucil is chosen as the model drug for the incorporation and release studies. Pure and drug-loaded nanoparticles are successfully prepared using various stabilizers (Polysorbate 80, Pluronic F68, Dextran 40). The nanoparticles coated with Polysorbate 80 are of highest interest since they could overcome the blood–brain barrier and the multidrug resistance in cancer cells. Such nanoparticles can be easily prepared by the nanoprecipitation approach reported here.
The colloidal particles of poly(alkyl cyanoacrylate) (PACA) posses a great promise as drug carrier systems for delivery of anticancer drugs, antibiotics and other pharmaceuticals. Such particles are classically prepared by emulsion polymerization, starting from the respective monomer. Our recent studies demonstrate that pure and drug-loaded PACA colloidal particles could be successfully prepared by nanoprecipitation, starting from a presynthesized polymer. In this report, we consider the advantages and disadvantages of both methods (nanoprecipitation and polymerization) for the preparation of PACA colloids, loaded with anticancer drugs. The effects of preparation method on the characteristics of as-obtained drug-loaded PACA colloids are described. The possibilities for application of such particles for cancer treatment are discussed.
Design, Development and Characterization of Econazole loaded Nanoparticles for Topical Application
INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE
Background and Objectives: Econazole nitrate (ECN) loaded nanoparticles with topical administration were the focus of the current study, which aimed to improve the topical efficacy of the medicine in treating fungal infections while also mitigating the drug’s gastrointestinal (GI) side effects. Further colloidal carrier methodology was employed as a method for the topical administration of medications with precision. Method: The emulsification-diffusion (E-D) method is an alternate approach for preparing nanogels that avoids the toxicitysolvent issues associated with the emulsification-evaporation technique. Its ease of use, enhanced stability, and adaptability have all been verified by a variety of research groups. ECN loaded with dichloromethane in stabilizer solution, formulated by high-speed homogenization at elevated pressure. The addition of aqueous phase with repeated homogenization cycles causes drug diffusion into nanogels. Further addition of mannitol as cryoprotectant and...
Indian Journal of Clinical Biochemistry, 2013
Emulsion polymerization was used to synthesize poly butyl cyanoacrylate nanoparticles in presence of steric stabilizer dextran 70. Nanoparticles were characterized by particle size analysis, scanning electron microscopy and light microscopy. Polymerization factors affecting particle size and distribution such as dextran 70, polysorbate 80 (PS 80) and H ? concentration, polymerization time and temperature, and sonication were studied. Distinct concentrations of stabilizer were needed to produce proper nanoparticles. In this case, the appropriate value was 2 % of total volume. At pH 4 significant decrease in production efficiency demonstrated the substantial effect of H ? concentration on nanoparticles. Furthermore significant increases in particle size and distribution was observed at 50°C compared to room temperature. 0.001 % (v/v) PS 80 represented notable influence on size and distribution. In addition, shaped nanoparticles were obtained by altering polymerization time from 5.5 h to 18 h. Finally, nanoparticle features were influenced by different factors. Appropriate manipulating of such factors can lead to obtaining desirable nanoparticles.
European Journal of Pharmaceutical Sciences, 2009
Curcumininoids, obtained from the rhizomes of Curcuma longa L., Zingiberaceae (turmeric), are the most widely used phytoconstituent in food industry and recently for its therapeutic activity. It has very wide spectrum of therapeutic use like in inflammation, psoriasis, various tumors, wound healing and also in neurodegenerative diseases like Alzheimer's disease. But its highly lipophilic nature and very poor bioavailability hampers its therapeutic usefulness. Poly(butyl) cyanoacrylate (PBCA) nanoparticles coated with poloxamer 188 containing curcuminoids were prepared by anionic polymerization using solvent evaporation method. The particle size and zeta potential of prepared liposomes was 178 nm and −28.33 respectively with 77.99% encapsulation efficiency. The TEM study revealed the spherical nature of the prepared nanoparticles alongwith confirmation of particle size. The polymerization and entrapment of curcuminoids was confirmed using H 1 NMR study by comparing the spectra of nanoparticles with that of curcuminoids. DSC study revealed that curcuminoids was entrapped inside the nanoparticles in molecular dispersion form. In vitro release study showed that the prepared PBCA nanoparticles are capable of controlled drug release (following matrix model) for extended period of time with higher release in acidic environment compared to PB 7.4 suggesting the usefulness of the prepared nanoparticles for intracellular delivery. The mean particle size, zeta potential and the amount of curcuminoids showed no significant changes compared to the freshly prepared PBCA nanoparticles after storage for 6 months at 40 • C/75% RH in the presence and absence of sunlight.
Formulation and Evaluation of Polymeric Nanoparticle by Nano-Precipitation Method
2020
Acyclovir is also known as Acyclovir, this drug is used for treatment of viral infection, particularly for treatment of herpes simplex viral infection. These are taken for month during treatment of herpes simplex viral infection. These are showing the action against all herps virus family. The acyclovir is poorly water-soluble drug. Due to that main aim is to increase the solubility of acyclovir in other solvent. The bioavailability of acyclovir is very less about (15-35%) because it has less oral route absorption. Due to that the acyclovir are given in intravenous route. When acyclovir is taken in oral route, the peak plasma concentration occurs after 1-2 h. The acyclovir having 9-33% of plasma protein binding. The BCS class of acyclovir are Class third (high solubility and Low permeability). Due to that acyclo vir are formulate in the form of nanoparticle. Chitosan are the polymers which are used for the formulation of nanoparticle. The chitosan is found to be compatible with acyc...
Influence of the preparation conditions on poly(ethylcyanoacrylate) nanocapsule formation
International Journal of Pharmaceutics, 1995
Poly(ethylcyanoacrylate) (PECA) nanocapsules suitable for use as drug delivery systems were prepared by in situ polymerization, adding the monomer to an organic phase and subsequent mixing of the latter to an aqueous phase containing a nonionic surfactant. Different preparation conditions have been able to influence the final PECA nanocapsule colloidal suspension. In particular, the kind of organic solvent caused the formation of either simple PECA nanocapsule suspensions (aprotic fully water-miscible solvents) or PECA nanoparticle colloidal suspensions consisting of nanospheres and nanocapsules (protic water-miscible solvent). Both mechanisms, the interracial precipitation of a pre-formed polymer and the interracial polymerization, could play a significant role in nanocapsule formation. Also other variables, such as the kind of the nonionic surfactant and the monomer concentration, affected in different ways the nanocapsule formation process.
Acta Biomaterialia, 2009
The design, preparation and characterization of poly(butylcyanoacrylate) nanoparticles as a drug-delivery system for daunorubicin is reported. A range of light scattering [photon correlation spectroscopy (PCS)], spectroscopic [1H nuclear magnetic resonance (1H NMR), Fourier transform infrared (FTIR), chromatographic [gel permeation chromatography (GPC)] and quantum chemical techniques have been employed for the physicochemical characterization of drug-loaded nanoparticles and to clarify the mechanisms of drug immobilization in the polymer matrix. The presence of daunorubicin in the polymerization medium was found to affect both the degree of polymerization and the compactness of the resulting nanoparticles. The GPC, FTIR and 1H NMR results confirmed cytostatic immobilization in the polymer matrix, with evidence for the presence of three types of inclusion: physically entrapped, polymer-associated (due to hydrogen bonds and/or dipole-charge interactions with the polymer chains), and polymer surface-adsorbed daunorubicin. The developed colloidal delivery system has the capacity for sustained in vitro release of daunorubicin. Preliminary in vitro assays were carried out on two cell lines, DLKP and DLKP-A, which display different levels of drug resistance, to evaluate the cytotoxicity of the drug-loaded nanoparticles.
African Journal of Pharmacy and Pharmacology, 2013
The main aim of the present work was to formulate anti-neoplastic drug loaded polymeric nanoparticles using biodegradable polymers (Chitosan and Eudragit RS 100) by emulsion droplet coalescence method. The model drug used here is 5-fluorouracil which is a pyrimidine analogue that is mainly used to treat colonic carcinoma, under the category of anti-neoplastic drugs. Tween 20 was used as emulsifier and colloidal stabilizer. The prepared nanoparticles were evaluated for particle size, surface morphology by TEM, surface charge, drug loading and entrapment efficiency, and for drug release by diffusion. Results show that the prepared nanoparticles are in nanosize, below 1000 nm, having appropriate zeta potential values with better entrapment of drug and controlled release of drug for a period of 12 h. From the obtained formulations, EF5 was selected as best with high entrapment efficiency, optimum zeta potential, and showing more controlled release of drug.