Preparation and characterization of biodegradable paclitaxel loaded alginate microparticles for pulmonary delivery (original) (raw)
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International Journal of Breast Cancer, 2016
Purpose. The antitumor activity of a novel alginate (ALG) polymer-based particle that contained paclitaxel (PTX) was evaluated using human primary breast cancer cells.Materials and Methods. PTX was combined with ALG in a nanoparticle as a drug delivery system designed to improve breast cancer tumor cell killing. PTX-ALG nanoparticles were first synthesized by nanoemulsification polymer cross-linking methods that improved the aqueous solubility. Structural and biophysical properties of the PTX-ALG nanoparticles were then determined by transmission electron microscopy (TEM) and high performance liquid chromatography (HPLC) fluorescence. The effect on cell cycle progression and apoptosis was determined using flow cytometry.Results. PTX-ALG nanoparticles were prepared and characterized by ultraviolet (UV)/visible (VIS), HPLC fluorescence, and TEM. PTX-ALG nanoparticles demonstrated increased hydrophobicity and solubility over PTX alone. Synthetically engineered PTX-ALG nanoparticles pro...
Preparation iiand characterization of mucoadhesive microcapsules of paclitaxel
International Journal of Research in Pharmaceutical Sciences, 2020
The objective of the present work was to develop paclitaxel encapsulated mucoadhesive microcapsules with an aim to enhance its efficacy and control the drug release in cancer patients. Paclitaxel microcapsules with a coat consisting of sodium alginate and mucoadhesive polymer such as acacia, Carbomer 941, Povidone K-30, Macrogol (PEG 6000) were prepared by ionotropic gelation technique and were evaluated for morphological characters, drug content, loading efficiency, drug–polymer interactions, swelling ratio, mucoadhesive properties and in vitro drug release. The resulting microcapsules were discrete, spherical, and free-flowing with a particle size range of 534 to 822 µm. The microencapsulation efficiency was 45.09–99.83%. The microcapsules prepared with alginate along with macrogol (F4M) have exhibited good mucoadhesive property in the in vitro wash off test. The swelling ratio of microcapsules was enhanced with increased alginate concentration and the formulation (F4) showed high...
DESIGN AND DEVELOPMENT OF PACLITAXEL -LOADED MICROSPHERES FOR TARGETED DRUG DELIVERY TO THE COLON
The purpose of this investigation was to prepare and evaluate the colon-specific microspheres of Paclitaxel for the treatment of colon cancer. Core microspheres of alginate were prepared by the modified emulsification method in liquid paraffin and by cross-linking with calcium chloride. The core microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach and small intestine. The microspheres were characterized by shape, size, surface morphology, size distribution, incorporation efficiency, and in vitro drug release studies. The outer surfaces of the core and coated microspheres, which were spherical in shape, were rough and smooth, respectively. The size of the core microspheres ranged from 20 to 52 µm, and the size of the coated microspheres ranged from 107 to 178 µm. The core microspheres sustained the drug release for 10 hours. The release studies of coated microspheres were performed in a pH progression medium mimicking the conditions of the gastrointestinal tract. Release was sustained for up to 20 hours in formulations with core microspheres to a Eudragit S-100 coat ratio of 1:7, and there were no changes in the size, shape, drug content, differential scanning calorimetry thermogram, and in vitro drug release after storage at 40°C/75% relative humidity for 6 months.
Indian Journal of Pharmaceutical Education and Research, 2022
Aim/background: Microspheres are spherical particles, having a core, having a particle size of 1μm to 1000μm. They are advantageous as compared to conventional dosage forms of drugs, in parameters like sustainability and control of drug release, drug protection, biodegradability, targeting ability and many more. Gemcitabine is a prodrug and is used in various carcinomas. Sodium Alginate and Ethyl Cellulose are used as polymers. The fabrication aims to sustain the drug release which can treat pancreatic, breast, ovarian and lung cancer. Materials and Methods: Microspheres have been made by Ionotropic Gelation method, Sodium alginate, Ethyl cellulose and Calcium chloride. Weighed quantity of drug and polymer were added to sodium alginate solution, which was then added drop wise to Calcium chloride solution under continuous stirring to procure spherical rigid microspheres. These were then subjected to various physicochemical characterizations and surface analysis. Results and Conclusio...
Sodium Alginate—Natural Microencapsulation Material of Polymeric Microparticles
International Journal of Molecular Sciences
From the multitude of materials currently available on the market that can be used in the development of microparticles, sodium alginate has become one of the most studied natural anionic polymers that can be included in controlled-release pharmaceutical systems alongside other polymers due to its low cost, low toxicity, biocompatibility, biodegradability and gelatinous die-forming capacity in the presence of Ca2+ ions. In this review, we have shown that through coacervation, the particulate systems for the dispensing of drugs consisting of natural polymers are nontoxic, allowing the repeated administration of medicinal substances and the protection of better the medicinal substances from degradation, which can increase the capture capacity of the drug and extend its release from the pharmaceutical form.
Brazilian Journal of Pharmaceutical Sciences, 2011
This study aimed to obtain site-specific and controlled drug release particulate systems. Some particulates were prepared using different concentrations of sodium alginate (Na-Alg) alone and others were formulated using different proportions of Na-Alg with hydroxypropyl methylcellulose (HPMC) stearoxy ether (60M viscosity grade), a hydrophobic form of conventional HPMC, using diclofenac potassium (DP) by ion-exchange methods. Beads were characterized by encapsulation efficiency, release profile, swelling, and erosion rate. The suitability of common empirical (zero-order, first-order and Higuchi) and semi-empirical (Ritger-Peppas and Peppas-Sahlin) models was studied to describe the drug release profile. The Weibull model was also studied. Models were tested by non-linear least-square curve fitting. A general purpose mathematical software (MATLAB) was used as an analysis tool. In addition, instead of the widely used linear fitting of log-transformed data, direct fitting was used to a...
International journal of pharmaceutics, 2018
In this study, we prepared paclitaxel (PTX) loaded bovine serum albumin (BSA) microparticles (MPs) of different sizes (0.5, 1.0, and 3.0 µm) and converted them into dry powders (DPs) of a uniform size (∼5.0 µm) through spray-drying techniques. The aim of preparing different sized PTX-MPs is to investigate the size-based in vivo biodistribution and retention of PTX in the lungs after intratracheal administration. Following the in vitro characterizations, the anti-tumor efficacy of the DPs containing differently sized PTX-BSA-MPs administered through intratracheal insufflation was compared with intravenously administered PTX solution (Taxol). While the fastest drug release was found for the 0.5 µm group, the 1.0 and 3.0 μm groups showed the highest anti-tumor efficiency in vivo. Taken together, our results demonstrate that the initial particle size of the incorporated particles, i.e., MPs, is crucial for the anti-tumor efficacy of DPs administered by inhalation, and the initial partic...
Doxorubicin hydrochloride (DOX) is used in treating ovarian, lung, and breast cancers. Its use in cancer chemotherapy is limited due to short plasma circulation, long elimination half-life, and non-specific cytotoxicity that may affect the normal cells. Thus, we have designed a drug delivery system, using a naturally occurring anionic polymer that is used for drug delivery due to its inert nature, high degree of biocompatibility, low toxicity, inexpensive and mild gelation with divalent cations such as calcium in forming particles. In this research, calcium alginate was used to encapsulate doxorubicin and assessed its compatibility with calcium alginate as drug delivery system. pH compatibility of alginate particle formation were assessed relative to the affinity of DOX. Alginate efficiency to encapsulate DOX was also tested and characterized through morphological analysis of the particles with the use of phase contrast microscope and scanning electron microscope (SEM). Fourier transform infrared spectrophotometer (FTIR) was used to confirm if the DOX was able to encapsulate within the alginate particles. Results showed that alginate encapsulation was compatible with DOX at neutral pH and encapsulation efficiency was achieved at 99.30%±0.0045 for 10ppm of DOX and 95.16%±0.011 for the 1.25ppm of DOX. An observable DOX-alginate particles with size average of 100-300μm using phase contrast microscope (40-60X magnification) and scanning electron microscope (200-300X magnification). DOX release in phosphate buffered saline (pH 7.2) confirmed that the DOX was successfully encapsulated based in FTIR data with comparable differences in the functional groups of DOX, alginate, and DOX released from the particles.
Alginate based Nanoparticles and Its Application in Drug Delivery Systems
Journal of Pharmaceutical Negative Results
Nanoparticulate systems made of biopolymers encompass promising properties as carriers and adjuvant for drug delivery. Alginate is one of the most widely investigated biomaterials in the field of nanoparticulate drug delivery due to its biodegradability, biocompatibility, and bioadhesivity. Alginate nanoparticles for drug delivery can be prepared through spray drying, ionic gelation, emulsification, covalent cross-linking, polyelectrolyte complexation, self-assembling, etc. Alginate is an extensively utilized biopolymer in multiple applications due to its gelling property and chemical structure with hydroxyl and carboxylate moieties. The biocompatibility, biodegradability of alginate, and solubility in water have broadened up research perspectives in material, and biomedical sciences. Study of alginate-based nanoparticles, nanoaggregates, and nanofibers initiated recently. In the present review, the physicochemical properties of alginate, which enabled its use as a pharmaceutical ex...
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Nanotechnology also called as nanotech is referring to the science, technology and engineering to synthesis, manipulation and investigation of materials and devices at nanoscales. Nanoparticles (NPs) owns a special place in nanotechnology due to their extreme-small size, multifunctionality, and modifiable surface for wide range of applications especially in new drug delivery application as the stability, solubility, biocompatibility and drugs releasing of NPs are highly controllable. The variation of nanomaterials with different physiochemical and morphological properties will affect the materials-living cells interaction and determination of the route of clearance and potential toxic effects. Thus, it requires more cross-disciplinary research on the designing and developing of drugs delivery NPs based on the diagnosis and treatment of devastating diseases. Biopolymers-based NPs have gained great attention for drug delivery system over the past few decades compared to other material...