Micro particles: An approach for betterment of drug delivery system

International Journal of Pharma Research and Development – Online 01/2011; 3(1):March/012.


Recent drug discovery using advanced techniques such as genomics, combinatorial chemistry, high
throughput screening and in silico three dimensional drug design has yielded drug candidates with low
water solubility and thus an inherently low mucosal permeability which makes the development of
pharmaceutical formulations difficult. To overcome these, particulate systems like microparticles have
been used as a physical approach to alter and improve the pharmacokinetic and pharmacodynamics
properties of various types of drug molecules. They have been used in vivo to protect the drug entity in
the systemic circulation, restrict access of the drug to the chosen sites and to deliver the drug at a
controlled and sustained rate to the site of action. Various polymers have been used in the formulation
of microparticles for drug delivery research to increase therapeutic benefit, while minimizing side
effects. The review embraces various aspects of microparticle formulations, characterization, effect of
their characteristics and their applications in delivery of drug molecules and therapeutic genes.

Download full-text


Available from: Mahesh Thube patil,
279 Reads
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: Objective The objective of the present investigation was to develop Glimepiride loaded cellulose acetate controlled release micro particulates.Methods The Glimepiride micro particles were prepared by emulsion solvent evaporation method. The effects of different parameters on the drug content and on the release of the drug from the micro particulates were investigated. Micro particulates were characterized in terms of encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis and drug release studies.ResultsAn increase in core:coat ratio from 1:1 to 1:3 caused an increase in the encapsulation efficiency and average particle size. FTIR and DSC studies exhibited there is no interaction between drug and excipients. The SEM studies clearly showed that the micro particles exhibited good spherical nature. The in vitro release of Glimepiride from micro particles in phosphate buffer of pH 7.8 was found to be dependent on molecular weight and copolymer type. The release kinetics of Glimepiride from optimized formulation followed zero order and peppas mechanism. The release exponent showed that the values of ‘n’ were between 0.95 and 1.07 indicating that the release from micro particulates was predominantly by non-fickian transport mechanism. The dissolution profiles of optimized formulation before and after stability studies were evaluated as per ICH guidelines.Conclusion The results demonstrate the feasibility of the model in the development of extended release dosage form.
    Drug Invention Today 09/2013; 5(3):235–240. DOI:10.1016/j.dit.2013.06.006
  • [Show abstract] [Hide abstract]
    ABSTRACT: The delivery of drugs through the oral route is regarded as most optimal to achieve desired therapeutic effects and patient compliance. However, poor pharmacokinetic profiles of oral drug candidates remains an area of concern, and approaches to enhance their bioavailability are widely cited in the literature. Traditionally, the approaches have been confined to molecular optimization of the drug molecule, which has gradually evolved into development of microsized and nanosized formulations. Nanoformulations, by virtue of their nanosize, are widely acclaimed for circumventing the obstacles of poor pharmacokinetics. In this review, an attempt has been made to discuss existing challenges of bioavailability and approaches to overcome the same, with in-depth compilation of the literature on nanoformulations. The nanoformulations reviewed include nanocrystals, nanoemulsions, polymeric nanoparticles, self-nanoemulsifying drug delivery systems, dendrimers, carbon nanotubes, polymeric micelles and lipid nanocarriers. This review confirms the potential of nanomedicines to improve the pharmacokinetics of drugs via nanoformulations. Chemotherapeutic applications and patent reports are also compiled in the review. Despite the promising benefits, nanomedicines are associated with hazards to human health. Hence, the review also deals with toxicological consequences of nanomedicines, and with in vitro/in vivo screening methods to assess bioavailability as per regulatory considerations. Nanotechnology has been shown to facilitate the clinical translation of drug candidates that were deemed to be bioavailability failures. Conclusively, nanotechnological approaches to particle design and formulation are beginning to expand the market for many drugs with improved bioavailability and therapeutics. However, dedicated efforts are needed to develop advanced nanomedicines with minimal or no adverse effects.
    Clinical Pharmacokinetics 01/2015; 54(4):325-357. DOI:10.1007/s40262-015-0242-x · 5.05 Impact Factor