TITLE

A Uniform Ultra-Small Microsphere/SAIB Hybrid Depot with Low Burst Release for Long-Term Continuous Drug Release

AUTHOR(S)
Lin, Xia; Xu, Yuhong; Tang, Xing; Zhang, Yan; Chen, Jian; Zhang, Yu; He, Haibing; Yang, Ziyi
PUB. DATE
November 2015
SOURCE
Pharmaceutical Research;Nov2015, Vol. 32 Issue 11, p3708
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Purpose: In the present study, a uniform ultra-small microsphere/sucrose acetate isobutyrate (SAIB) hybrid depot (m-SAIB depot) was designed to provide a long-term sustained release drug delivery system which not only reduced the burst release of an SAIB depot, but also eliminated the lag-time of PLGA microspheres. Methods: Risperidone loaded m-SAIB depot (Ris-m-SAIB depot) was characterized by in vitro drug release, pharmacokinetics, in vivo degradation and biocompatibility, in comparison with risperidone loaded SAIB depot (Ris-SAIB depot). Results: Ris-m-SAIB depot showed a low burst release (0.64%) and a reduced in vitro drug release rate due to the encapsulation of most drug in microspheres. After intramuscular administration, the in vivo burst release of Ris-m-SAIB was significantly decreased, as reflected by the low C/C (approximately 30-fold reduction), in comparison with Ris-SAIB depot. From 4 to 78 days, Ris-m-SAIB depot showed a higher plasma drug level (1.55 ~ 16.30 ng/ml) with a steadier drug release profile compared with Ris-SAIB depot. Ris-m-SAIB depot degraded gradually with a degradation t of 54.6 days and exhibited good biocompatibility in vivo. Conclusion: These results demonstrate the potential application of a uniform ultra-small microsphere/SAIB hybrid depot for continuously delivering small drug molecules for long periods of time without burst release.
ACCESSION #
110202843

 

Related Articles

  • Docetaxel-Loaded Chitosan Microspheres as a Lung Targeted Drug Delivery System: In Vitro and in Vivo Evaluation. Hao Wang; Yongdong Xu; Xiao Zhou // International Journal of Molecular Sciences;Mar2014, Vol. 15 Issue 3, p3519 

    The aim of this study was to prepare docetaxel-loaded chitosan microspheres and to evaluate their in vitro and in vivo characteristics. Glutaraldehyde crosslinked microspheres were prepared using a water-in-oil emulsification method, and characterized in terms of the morphological examination,...

  • Nanocarriers for Biomedical Applications. Shuyi Li; Lynsa Nguyen; Hairong Xiong; Meiyao Wang; Hu, Tom C.-C.; Jin-Xiong She; Serkiz, Steven M.; Wicks, George G.; Dynan, William S. // Journal of the South Carolina Academy of Science;2011, Vol. 9 Issue 1, p30 

    Porous-wall hollow glass microspheres (PW-HGMs) show promise for drug delivery applications. They are a novel ceramic biocompatible material with a hollow central cavity surrounded by a thin mesoporous shell. The central cavity can be loaded with a high concentration of a soluble biological...

  • Tuning Pharmacokinetics and Biodistribution of a Targeted Drug Delivery System Through Incorporation of a Passive Targeting Component. Kudgus, Rachel A.; Walden, Chad A.; McGovern, Renee M.; Reid, Joel M.; David Robertson, J.; Mukherjee, Priyabrata // Scientific Reports;7/11/2014, p1 

    Major challenges in the development of drug delivery systems (DDSs) have been the short half-life, poor bioavailability, insufficient accumulation and penetration of the DDSs into the tumor tissue. Understanding the pharmacokinetic (PK) parameters of the DDS is essential to overcome these...

  • Carbon Nanotubes as an Advanced Drug and Gene Delivery Nanosystem. Dolatabadi, Jafar Ezzati Nazhad; Omidi, Yadollah; Losic, Dusan // Current Nanoscience;Jun2011, Vol. 7 Issue 3, p297 

    New nanomaterials have been extensively explored in recent years for drug delivery applications to address problems associated with the conventional drug therapies such as limited drug solubility, poor biodistribution, lack of selectivity and unfavourable pharmacokinetics. Among them, carbon...

  • Design and development of chronopharmaceutical drug delivery of simvastatin. Sukanya, M.; Kishore, V. Sai // Journal of Chemical & Pharmaceutical Research;2012, Vol. 4 Issue 6, p3195 

    The aim of the present investigation is to develop a pulsatile drug delivery system basedon an insoluble capsule body filled with simvastatin microspheres and sealed with HPMCK4M plug. Simvastatin is a water insoluble drug and its absorption is dissolution rate limited. Hence simvastatin...

  • Optimization of Eudragit RS Microspheres for controlled release of Theophylline using Response Surface Methodology. M.El-Nahas, Hanan // Journal of Pharmaceutical Sciences & Research;2010, Vol. 2 Issue 10, p663 

    The present study reports on the production of theophylline loaded Eudragit RS microspheres for controlled release. The microspheres were prepared by the emulsion solvent evaporation technique using Eudragit RS as the polymer. A three-factor, three-level design of experiment (DOE) with response...

  • Biocompatibility and Degradation of Theophylline/Chitosan Microspheres as Pulmonary Delivery Carriers. Zhanqin Feng; Juanjuan Cui; Xueping Huang; Yuqing Sun; Zengjuan Zheng; Weifen Zhang // Advanced Materials Research;2014, Issue 934, p199 

    The purpose of this study was to investigate the biocompatibility and degradation behavior of theophylline/chitosan microspheres, which has the potential application in pulmonary delivery system. Hemolysis test was carried out to estimate its blood toxicity. In vitro enzymatic hydrolysis was...

  • Desloratadine Demonstrates Dose Proportionality in Healthy Adults After Single Doses. Gupta, S.; Banfield, C.; Affrime, M.; Marco, A.; Cayen, M.; Herron, J.; Padhi, D. // Clinical Pharmacokinetics;2002 Supplement, Vol. 41 Issue 10, p1 

    Objective: To evaluate the dose proportionality and linearity and pharmacokinetic profile of desloratadine after single oral doses over the range of 5 to 20mg. Design: Single centre, randomised, open-label, 4-way crossover study in which healthy adults received single doses of desloratadine (5,...

  • Pegylation: a novel process for modifying pharmacokinetics. Harris, J.M.; Martin, N.E.; Modi, M. // Clinical Pharmacokinetics;2001, Vol. 40 Issue 7, p539 

    The use of liposomal carriers and the modification of therapeutic molecules through the attachment of poly(ethylene glycol) [PEG] moieties (‘pegylation’) are the most common approaches for enhancing the delivery of parenteral agents. Although ‘classical’ liposomes (i.e....

Share

Read the Article

Courtesy of THE LIBRARY OF VIRGINIA

Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics