Drug-Loaded Pectin Microparticles Prepared by Emulsion-Solvent Evaporation

2012 ◽  
Vol 506 ◽  
pp. 282-285 ◽  
Author(s):  
Pornsak Sriamornsak ◽  
S. Konthong ◽  
K. Burapapadh ◽  
Srisagul Sungthongjeen
Keyword(s):  
Crystalline State ◽  
Amorphous Solid ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Amorphous Solid Dispersion ◽  
Degree Of Esterification ◽  
X Ray ◽  
Evaporation Technique ◽  
Model Drug ◽  
High Degree

The aim of this study was to develop the pectin-based microparticles by emulsion-solvent evaporation technique. The effects of concentration and type of pectin and addition of glutaraldehyde on size, size distribution, drug crystalline state and drug dissolution from microparticles were investigated. The results showed that a model drug, indomethacin, could be encapsulated in microparticles. Higher molecular weight of pectin caused a larger in size of microparticles than the lower one. A high degree of esterification is preferred to stabilize the pectin microparticles. The powder x-ray diffractograms showed that all microparticles led to amorphous products while their physical mixture still showed the crystalline state of drug. Drug dissolution from the microparticles containing indomethacin and pectin was increased, resulting from the formation of an amorphous solid dispersion. Addition of glutaraldehyde, however, resulted in slower drug dissolution, compared to the formulations without glutaraldehyde or drug alone.

scholarly journals The Influence of Drug–Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticles

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 917
Author(s):  
Nele-Johanna Hempel ◽  
Padryk Merkl ◽  
Matthias Manne Knopp ◽  
Ragna Berthelsen ◽  
Alexandra Teleki ◽  
...  
Keyword(s):  
Laser Radiation ◽  
Near Infrared ◽  
Amorphous Solid ◽  
Plasmonic Nanoparticles ◽  
Drug Dissolution ◽  
Amorphous Solid Dispersion ◽  
Polymer Solubility ◽  
Model Drug ◽  
Final Dosage Form

In this study, laser-induced in situ amorphization (i.e., amorphization inside the final dosage form) of the model drug celecoxib (CCX) with six different polymers was investigated. The drug–polymer combinations were studied with regard to the influence of (i) the physicochemical properties of the polymer, e.g., the glass transition temperature (Tg) and (ii) the drug–polymer solubility on the rate and degree of in situ drug amorphization. Compacts were prepared containing 30 wt% CCX, 69.25 wt% polymer, 0.5 wt% lubricant, and 0.25 wt% plasmonic nanoparticles (PNs) and exposed to near-infrared laser radiation. Upon exposure to laser radiation, the PNs generated heat, which allowed drug dissolution into the polymer at temperatures above its Tg, yielding an amorphous solid dispersion. It was found that in situ drug amorphization was possible for drug–polymer combinations, where the temperature reached during exposure to laser radiation was above the onset temperature for a dissolution process of the drug into the polymer, i.e. TDStart. The findings of this study showed that the concept of laser-induced in situ drug amorphization is applicable to a range of polymers if the drug is soluble in the polymer and temperatures during the process are above TDStart.

Development of Nifedipine Amorphous Solid Dispersion Composed of Surface-Active Agents

2021 ◽  
Vol 901 ◽  
pp. 35-39
Author(s):  
Sukannika Tubtimsri ◽  
Yotsanan Weerapol
Keyword(s):  
Surface Active Agent ◽  
Active Agent ◽  
Amorphous Solid ◽  
Drug Dissolution ◽  
Amorphous Solid Dispersion ◽  
Polysorbate 80 ◽  
X Ray ◽  
Surface Active Agents ◽  
Surface Active ◽  
Methacrylate Copolymer

The amorphous solid dispersions (ASDs) containing amino methacrylate copolymer and surface-active agents were prepared to improve the nifedipine (NDP) dissolution. The different types of surface-active agent i.e., polysorbates 80, sodium lauryl sulfate (SLS) and polyethylene glycol (PEG) 400 were used. In order to evaluate the ASDs formulation,powder X-ray diffractometry and thermal analysis to characterize NDP crystallinity in ASDs and the dissolution study of NDP have been performed to compare the dissolution profiles. The ASDs were kept for 6 months to investigate the stability. In the X-ray diffraction pattern, no peak was observed in all samples of ASDs. No peak was found in sample of all ASDs from the thermograms. These results suggest that the drug may be molecularly dispersed in matrix of amino methacrylate copolymer. The drug dissolution at 120 min, from ASDs without surface-active agent and NDP powder were 58.31% and 17.95%, respectively. The dissolved NDP from ASDs composed of SLS, polysorbate 80 and PEG400 were 96.25%, 88.86% and 75.32%, respectively. These results may occur due to the reduction of surface tension, the addition of the low amount of high efficiency of surface-active agent e.g., SLS (compared with PEG400 and polysorbate 80) provided the higher NDP dissolution. The content analysis of NDP in selected ASDs was studied at the end of 3 and 6 months, the NDP content remained unchanged after storage.

scholarly journals Influence of Drug Load on the Printability and Solid-State Properties of 3D-Printed Naproxen-Based Amorphous Solid Dispersion

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4492
Author(s):  
Eric Ofosu Kissi ◽  
Robin Nilsson ◽  
Liebert Parreiras Nogueira ◽  
Anette Larsson ◽  
Ingunn Tho
Keyword(s):  
Solid State ◽  
3D Printing ◽  
Solid Dispersion ◽  
Physical Stability ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersion ◽  
Drug Load ◽  
X Ray ◽  
3D Printed ◽  
Hot Melt

Fused deposition modelling-based 3D printing of pharmaceutical products is facing challenges like brittleness and printability of the drug-loaded hot-melt extruded filament feedstock and stabilization of the solid-state form of the drug in the final product. The aim of this study was to investigate the influence of the drug load on printability and physical stability. The poor glass former naproxen (NAP) was hot-melt extruded with Kollidon® VA 64 at 10–30% w/w drug load. The extrudates (filaments) were characterised using differential scanning calorimetry (DSC), dynamic mechanical analysis (DMA), and thermogravimetric analysis (TGA). It was confirmed that an amorphous solid dispersion was formed. A temperature profile was developed based on the results from TGA, DSC, and DMA and temperatures used for 3D printing were selected from the profile. The 3D-printed tablets were characterised using DSC, X-ray computer microtomography (XµCT), and X-ray powder diffraction (XRPD). From the DSC and XRPD analysis, it was found that the drug in the 3D-printed tablets (20 and 30% NAP) was amorphous and remained amorphous after 23 weeks of storage (room temperature (RT), 37% relative humidity (RH)). This shows that adjusting the drug ratio can modulate the brittleness and improve printability without compromising the physical stability of the amorphous solid dispersion.

scholarly journals The Development and Optimization of Hot-Melt Extruded Amorphous Solid Dispersions Containing Rivaroxaban in Combination with Polymers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 344
Author(s):  
Jong-Hwa Lee ◽  
Hyeong Sik Jeong ◽  
Jong-Woo Jeong ◽  
Tae-Sung Koo ◽  
Do-Kyun Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Oral Drug Delivery ◽  
Amorphous Solid ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Amorphous Solid Dispersion ◽  
Screw Speed ◽  
Hot Melt

Rivaroxaban (RXB), a novel oral anticoagulant that directly inhibits factor Xa, is a poorly soluble drug belonging to Biopharmaceutics Classification System (BCS) class II. In this study, a hot-melt extruded amorphous solid dispersion (HME-ASD) containing RXB is prepared by changing the drug:polymer ratio (Polyvinylpyrrolidione-vinyl acetate 64, 1:1–1:4) and barrel temperature (200–240 °C), fixed at 20% of Cremophor® RH 40 and 15 rpm of the screw speed, using the hot-melt extruding technique. This study evaluates the solubility, dissolution behavior, and bioavailability for application to oral drug delivery and optimizes the formulation of rivaroxaban amorphous solid dispersion (RXB-ASD). Based on a central composite design, optimized RXB-ASD (PVP VA 64 ratio 1:4.1, barrel temperature 216.1 °C, Cremophor® RH 40 20%, screw speed 15 rpm) showed satisfactory results for dependent variables. An in vitro drug dissolution study exhibited relatively high dissolution in four media and achieved around an 80% cumulative drug release in 120 min. Optimized RXB-ASD was stable under the accelerated condition for three months without a change in crystallinity and the dissolution rate. A pharmacokinetic study of RXB-ASD in rats showed that the absorption was markedly increased in terms of rate and amount, i.e., the systemic exposure values, compared to raw RXB powder. These results showed the application of quality by design (QbD) in the formulation development of hot-melt extruded RXB-ASD, which can be used as an oral drug delivery system by increasing the dissolution rate and bioavailability.

scholarly journals Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Irin Dewan ◽  
Swarnali Islam ◽  
Md. Sohel Rana
Keyword(s):  
Drug Release ◽  
Promising Result ◽  
Release Kinetics ◽  
Type Ii Diabetes Mellitus ◽  
Solvent Evaporation ◽  
Ftir Studies ◽  
Evaporation Technique ◽  
Model Drug

The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and erosion as the correlation coefficient (R2) best fitted with Korsmeyer model and release exponent (n) was 0.45–0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

Fabrication of Nanocolorants Using Miniemulsion Solvent Evaporation Technique

2013 ◽  
Vol 785-786 ◽  
pp. 471-474
Author(s):  
Xiao Zhao ◽  
Shan Xu ◽  
Gao Zhan Xie
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Light Scattering ◽  
Photoelectron Spectroscopy ◽  
Solvent Evaporation ◽  
Dye Molecules ◽  
X Ray ◽  
Transmission Electron ◽  
Evaporation Technique ◽  
Formulation Variables

The combined miniemulsion and solvent evaporation (MESE) method was employed to fabricate hydrophobic dye/polymer composite colorants in the present work. Using dynamic light scattering tests, the effect of the formulation variables on the size and size distribution of the prepared nanoparticles was examined. Transmission electron microscopy, UVvisible spectrophotometry, X-ray photoelectron spectroscopy, and elemental analysis results indicate that dye molecules or aggregates were successfully encapsulated in the poly (methyl methacrylate) matrix using the MESE method and the resulting composite colorant could be dispersed in water.

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