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      Microencapsulation: A promising technique for controlled drug delivery

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          Abstract

          Microparticles offer various significant advantages as drug delivery systems, including: (i) an effective protection of the encapsulated active agent against (e.g. enzymatic) degradation, (ii) the possibility to accurately control the release rate of the incorporated drug over periods of hours to months, (iii) an easy administration (compared to alternative parenteral controlled release dosage forms, such as macro-sized implants), and (iv) Desired, pre-programmed drug release profiles can be provided which match the therapeutic needs of the patient. This article gives an overview on the general aspects and recent advances in drug-loaded microparticles to improve the efficiency of various medical treatments. An appropriately designed controlled release drug delivery system can be a foot ahead towards solving problems concerning to the targeting of drug to a specific organ or tissue, and controlling the rate of drug delivery to the target site. The development of oral controlled release systems has been a challenge to formulation scientist due to their inability to restrain and localize the system at targeted areas of gastrointestinal tract. Microparticulate drug delivery systems are an interesting and promising option when developing an oral controlled release system. The objective of this paper is to take a closer look at microparticles as drug delivery devices for increasing efficiency of drug delivery, improving the release profile and drug targeting. In order to appreciate the application possibilities of microcapsules in drug delivery, some fundamental aspects are briefly reviewed.

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          Most cited references109

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          Chitosan: a unique polysaccharide for drug delivery.

          The aim of this review is to give an insight into the many potential applications of chitosan as a pharmaceutical drug carrier. The first part of this review concerns the principal uses of chitosan as an excipient in oral formulations (particularly as a direct tableting agent) and as a vehicle for parenteral drug delivery devices. The use of chitosan to manufacture sustained-release systems deliverable by other routes (nasal, ophthalmic, transdermal, and implantable devices) is discussed in the second part.
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            Polymer-drug compatibility: a guide to the development of delivery systems for the anticancer agent, ellipticine.

            To establish a method for predicting polymer-drug compatibility as a means to guide formulation development, we carried out physicochemical analyses of polymer-drug pairs and compared the difference in total and partial solubility parameters of polymer and drug. For these studies, we employed a range of biodegradable polymers and the anticancer agent Ellipticine as the model drug. The partial and total solubility parameters for the polymer and drug were calculated using the group contribution method. Drug-polymer pairs with different enthalpy of mixing values were analyzed by physicochemical techniques including X-ray diffraction and Fourier transform infrared. Polymers identified to be compatible [i.e., polycaprolactone (PCL) and poly-beta-benzyl-L-aspartate (PBLA)] and incompatible [i.e., poly (d,l-lactide (PLA)], by the above mentioned methods, were used to formulate Ellipticine. Specifically, Ellipticine was loaded into PBLA, PCL, and PLA films using a solvent casting method to produce a local drug formulation; while, polyethylene oxide (PEO)-b-polycaprolactone (PCL) and PEO-b-poly (d,l-lactide) (PLA) copolymer micelles were prepared by both dialysis and dry down methods resulting in a formulation for systemic administration. The drug release profiles for all formulations and the drug loading efficiency for the micelle formulations were also measured. In this way, we compared formulation characteristics with predictions from physicochemical analyses and comparison of total and partial solubility parameters. Overall, a good correlation was obtained between drug formulation characteristics and findings from our polymer-drug compatibility studies. Further optimization of the PEO-b-PCL micelle formulation for Ellipticine was also performed. Copyright 2004 Wiley-Liss, Inc.
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              Polyphosphoesters in drug and gene delivery.

              Polymers with repeating phosphoester bonds in the backbone are structurally versatile, and biodegradable through hydrolysis, and possibly enzymatic digestion at the phosphoester linkages under physiological conditions. These biodegradable polyphosphoesters are appealing for biological and pharmaceutical applications because of their potential biocompatibility and similarity to bio-macromolecules such as nucleic acids. In the first part of this review, we will focus on one particular structure synthesized by extending oligomeric lactide prepolymers with ethylphosphate groups. This amorphous to semi-crystalline polymer is promising in delivering anti-cancer therapeutics in the form of microspheres. In the second half, we will discuss the conjugation of charged groups to the side chain of the phosphate, constituting one of the few biodegradable cationic polymers in the field for non-viral gene delivery. Capable of delivering exogenous genes to a cell nucleus or providing an extracellular sustained release of DNA, these cationic polyphosphoesters also serve as a valuable model to understand the important characteristics that render a polymer an effective gene carrier.
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                Author and article information

                Journal
                Res Pharm Sci
                JJRPS
                Research in Pharmaceutical Sciences
                Medknow Publications (India )
                1735-5362
                1735-9414
                Jul-Dec 2010
                : 5
                : 2
                : 65-77
                Affiliations
                Department of Pharmaceutics, JSS College of Pharmacy, SS Nagar, Mysore, Karnataka-570015, India
                Author notes
                *Corresponding author: Hemant KSY Tel. 0091 9886112637 Email: haisunny2@ 123456yahoo.co.in
                Article
                JRPS-5-65
                3093624
                21589795
                9f122e8c-70a0-4d1e-896f-d6f5eaba12ed
                © Journal of Research in Pharmaceutical Sciences

                This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : July 2010
                : September 2010
                Categories
                Review Article

                Pharmacology & Pharmaceutical medicine
                controlled release,drug delivery systems,microencapsulation,microcapsules

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