scholarly journals Development and optimization of oil-filled lipid nanoparticles containing docetaxel conjugates designed to control the drug release rate in vitro and in vivo

2011 ◽  
pp. 2545 ◽  
Author(s):  
Rahima Benhabbour ◽  
Feng ◽  
Wu ◽  
Ma ◽  
Russell Mumper
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Lipid Nanoparticles ◽  
Drug Release Rate

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

STUDY OF THE DIFFERENT RELEASE CHARACTERISTICS OF ANTIBIOTICS FROM PATIENTS: A DYNAMIC ELUTING SYSTEM TO INVESTIGATE DRUG RELEASE FROM ANTIBIOTIC-IMPREGNATED CALCIUM SULFATE DELIVERY

2015 ◽  
Vol 15 (01) ◽  
pp. 1550012
Author(s):  
YANG ZHANG ◽  
RENJIE WU ◽  
YING HU ◽  
YU DONG ◽  
LIFENG SHEN ◽  
...  
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Release Rate ◽  
Calcium Sulfate ◽  
Fickian Diffusion ◽  
Release Behavior ◽  
Cumulative Release ◽  
In Vivo Release

Background: Antibiotic-impregnated calcium sulfate delivery systems (ACDS) are commonly used to treat chronic osteomyelitis. Our research is to investigate drug release in vitro over a longer period, as a cautious predictor of in vivo release. Methods: The local release behavior of antibiotic in vitro was simulated. The consecutive dynamic eluting experiment was performed based on the pro-operative characteristic of osteomyelitis patients and the determined results of drug concentration in the human drainage tissue fluid (DTF). The concentration of each drug in the receiving solution was detected by ultra-performance liquid chromatography-tandem quadrupole detector mass spectrometry. The ACDS was reviewed by scanning electronic microscopy (SEM) after 48 h, and prepared to be eluted for another examination after 33 days. The mechanism of antibiotic release was analyzed by using the Ritger–Peppas and Weibull equations. Results: The cumulative release rate of vancomycin in a vancomycin-calcium sulfate delivery system (VCDS) was 77.50 % (3.0 mm diameter) and 72.43 % (4.8 mm diameter), while that of the tobramycin in a tobramycin-calcium sulfate delivery system (TCDS) was 88.0 % (3.0 mm diameter) and 84.55 % (4.8 mm diameter). At the 15th day, approximately 27.92% of vancomycin was and 29.35% of tobramycin was released from the local implant in vivo. Using SEM, numerous vancomycin and tobramycin particles were found to be attached to the columnar calcium sulfate crystals at the start of the experiment. The release behavior of the two antibiotics followed a combination of Fickian diffusion and Case II transport mechanisms within the first 48 h, and a Fickian diffusion mechanism during the subsequent time period. The correlation coefficient of tobramycin and vancomycin in vivo and in vitro was 0.9704–0.9949 and 0.9549–0.9782, respectively. Conclusion: A good correlation of the in vivo and in vitro cumulative release rates was observed by comparing the cumulative release rate of drugs in vitro by means of the dynamic eluting model, and in the DTF. Therefore, our study has proved that it is possible to use the dynamic eluting model as a cautious predictor of in vivo release.

Effects of Four Mesostructures on their Drug Release Properties

2013 ◽  
Vol 645 ◽  
pp. 125-128
Author(s):  
Wei Zeng
Keyword(s):  
Drug Release ◽  
Mesoporous Materials ◽  
Release Rate ◽  
Drug Efficacy ◽  
Drug Release Rate ◽  
Ordered Mesoporous Materials ◽  
Ordered Mesoporous ◽  
Fast Release ◽  
Mcm 41

Five ordered mesoporous materials, SBA-1, MCM-48, SBA-7, MCM-41 and SBA-15, were prepared and tested as mesophase drug delivery systems with an anti-inflammatory drug, ibuprofen. The results of these mesostructures on in vitro ibuprofen delivery indicated that the mesoporous materials with cage-like structure, SBA-1 and SBA-7, had unfavorable load and release properties. MCM-48 also showed fast release rate due to its opening channel. However, the hexagonal mesostructure in MCM-41 and SAB-15 was advantageous for extending drug release rate although a little difference existed between them. Compared with commercial ibuprofen capsule, the release system based on MCM-41 materials displayed the drug efficacy in a longer time.

Development of Acrylic Matrix Type Ketoprofen Patch

2012 ◽  
Vol 506 ◽  
pp. 533-536
Author(s):  
Nanthida Wonglertnirant ◽  
S. Tipwichai ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Pressure Sensitive Adhesive ◽  
Drug Release Rate ◽  
Matrix Type ◽  
Adhesive Matrix ◽  
Pressure Sensitive ◽  
Transdermal Patches ◽  
Significant Difference

Ketoprofen transdermal patches (KTPs) were fabricated using an acrylic pressure sensitive adhesive (PSA) polymer. The influence of different factors (amount of PSA, drug content, and pressure applying on the backing membrane during preparation) on the characteristics of ketoprofen patch (thickness, W/A ratio, and adhesiveness of matrix film) and in vitro drug release behavior were investigated. The results revealed the successful fabrication and a good physical appearance of KTPs using acrylic PSA. Microscopic observations, FTIR spectra, and DSC thermograms were permitted to demonstrate that the drug was dispersed molecularly in the polymer. As the amount of PSA in the adhesive matrix was increased, the release rate of ketoprofen was decreased. Contrarily, the drug release rate was increased corresponding to the increase of ketoprofen content in the adhesive matrix. There was no significant difference in the release rate when the pressure applying on the backing membrane was varied. The kinetic of ketoprofen release from acrylic matrix type transdermal patches followed the Higuchis diffusion model.

Fig. 12 Scanning electron micrograph of D.L-PLA nanoparticles loaded with CGP 57813. (Ref. 51.) scanning force microscopy (also called atomic force microscopy), enable the visualiza-tion of nanoparticles at atmospheric pressure without gold coating [12,64]. Neverthe-less, the resolution obtained with these new tools is still lower than that with SEM. For size determination, transmission electron microscopy is not as widely used as PCS and SEM, but it is still a powerful method for determining the morphology of particles. With this technique, Fessi et al. [42] estimated the wall thickness of PLA nanocapsules. Krause et al. [18] described the highly porous structure of PLA nano-spheres prepared by the emulsion-evaporation procedure. VIII. IN VITRO RELEASE STUDIES In vitro release studies should in principle be useful for quality control as well as for the prediction of in vivo kinetics. Unfortunately, due to the very small size of the par-ticles, the release rate observed in vivo can differ greatly from the release obtained in a buffer solution. However, in vitro release studies remain very useful for quality control as well as for evaluation of the influence of process parameters on the release rate of active compounds. In vitro drug release from microdispersed systems has been exten-sively reviewed by Washington [65]. Depending on the type of polyester, drug release from nanoparticles can take place through several processes, of which the following appear to be the most important: (1) The drug may diffuse out of the carrier through the solid matrix; to allow complete release from the carriers, (the concentration of drug in the release medium should re-main infinitely low, which condition is known as sink condition); (2) The solvent may penetrate the nanoparticles and dissolve the drug, which then diffuses out into the re-lease medium. Depending on the physico-chemical characteristics of the particles, wa-ter can enter the particles through narrow pores or by hydration. Once the drug is dis-solved, the drug diffuses out of the particles. Here again, since diffusion is driving the

1998 ◽  
pp. 204-216
Keyword(s):  
Quality Control ◽  
Drug Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Scanning Force Microscopy ◽  
Force Microscopy ◽  
Release Studies ◽  
Vitro Release

scholarly journals A Rapid Dual-Responsive Releasing Nano-Carrier by Decomposing the Copolymer and Reversing the Core Dissolution

2021 ◽  
Vol 9 ◽  
Author(s):  
Sen Liu ◽  
Can Shen ◽  
Cheng Qian ◽  
Jianquan Wang ◽  
Zhihao Wang ◽  
...  
Keyword(s):  
Drug Release ◽  
Disulfide Bonds ◽  
Water Soluble ◽  
Drug Release Rate ◽  
The Core ◽  
Dual Responsive ◽  
Dual Response ◽  
Effective Drugs

The accumulation of nanotechnology-based drugs has been realized in various ways. However, the concentration of drugs encapsulated by nanomaterials is not equal to the concentration of effective drugs; often, the drugs become effective only when they are released from the nanomaterials as free drugs. This means only when the drugs are rapidly released after the accumulated drug-encapsulating nanomaterials can they truly achieve the purpose of increasing the concentration of drugs in the tumor. Therefore, we herein report a dual-response nano-carrier of glutathione and acid to achieve the rapid release of encapsulated drug and increase the effective drug concentration in the tumor. The nano-carrier was constructed using a dual-responsive amphiphilic copolymer, composed of polyethylene glycol and hydrophobic acetylated dextran and connected by a disulfide bond. In the tumor microenvironment, disulfide bonds could be biodegraded by glutathione that is overexpressed in the tumor, exposing the core of nano-carrier composed of acetylated dextran. Then the acidic environment would induce the deacetylation of acetylated dextran into water-soluble dextran. In this way, the nano-carrier will degrade quickly, realizing the purpose of rapid drug release. The results showed that the drug release rate of dual-responsive nano-carrier was much higher than that of glutathione or acid-responsive nano-carrier alone. Furthermore, both in vitro and in vivo experiments confirmed that dual-responsive nano-carrier possessed more efficient anti-tumor effects. Therefore, we believe that dual-responsive nano-carriers have better clinical application prospects.

scholarly journals Drug release rate in vitro and bioavailability of new controlled release suspension of spherical matrix of ibuprofen.

1989 ◽  
Vol 4 (2) ◽  
pp. 100-104
Author(s):  
Yoshiaki Kawashima ◽  
Taro Iwamoto ◽  
Toshiyuki Niwa ◽  
Hirofumi Takeuchi ◽  
Tomoaki Hino ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate

scholarly journals A Correlative Model to Predict In Vivo AUC for Nanosystem Drug Delivery with Release Rate-Limited Absorption

2012 ◽  
Vol 15 (4) ◽  
pp. 583 ◽  
Author(s):  
Mohammad Barzegar-Jalali ◽  
Kaivan Mohammadi ◽  
Ghobad Mohammadi ◽  
Hadi Valizadeh ◽  
Azim Barzegar-Jalali ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Biological Action ◽  
Theoretical Justification ◽  
In Vitro Drug Release ◽  
Proposed Model ◽  
Gaining Insight

Purpose. Drug release from nanosystems at the sites of either absorption or effect biophase is a major determinant of its biological action. Thus, in vitro drug release is of paramount importance in gaining insight for the systems performance in vivo. Methods. A novel in vitro in vivo correlation, IVIVC, model denoted as double reciprocal area method was presented and applied to 19 drugs from 55 nano formulations with total 336 data, gathered from literature. Results. The proposed model correlated the in vitro with in vivo parameters with overall error of 12.4 ± 3.9%. Also the trained version of the model predicted the test formulations with overall error of 15.8 ± 3.7% indicating the suitability of the approach. A theoretical justification was provided for the model considering the unified classical release laws. Conclusion. The model does not necessitate bolus intravenous drug data and seems to be suitable for IVIVC of drugs with release rate-limited absorption. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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