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[email protected] 1. INTRODUCTION 1.1 NOVEL DRUG DELIVERY SYSTEM: The method by which a drug is delivered can have a significant effect on its efficacy. Some drugs have an optimum concentration range within which maximum benefit is derived, and concentrations above or below this range can be toxic or produce no therapeutic benefit at all. On the other hand, the very slow progress in the efficacy of the treatment of severe diseases, has suggested a growing need for a multidisciplinary approach to the delivery of therapeutics to targets in tissues. From this, new ideas on controlling the pharmacokinetics, pharmacodynamics, non-specific toxicity, immunogenicity, biorecognition, and efficacy of drugs were generated. These new strategies, often called drug delivery systems (DDS), are based on interdisciplinary approaches that combine polymer science, pharmaceutics, bioconjugate chemistry, and molecular biology. API Delivery CHEMISTRY PHARMACEUTICS PHARMACOLOGY PHARMACOGNOSY PHARMA. ANALYSIS CLINICAL RESEARCH BIOCHEMISTRY BIOTECHNOLOGY MISCELLANEOUS SUBSCRIBE WITH US Enter y o ur em ail addres s : Subscribe D o N o t Fo rget to V erify (C lic k o n S u b s c rip tio n lin k in yo ur inbo x ) LATEST ISSUE - DEC 14 Customized targeted API delivery work with each individual client REFERENCE ID: PHARMATUTOR-ART-1652 To minimize drug degradation and loss, to prevent harmful side-effects and to increase drug bioavailability and the fraction of the drug accumulated in the required zone, various drug delivery and drug targeting systems are currently under development. Among drug carriers one can name soluble polymers, microparticles made of insoluble or biodegradable natural and synthetic polymers, microcapsules, cells, cell ghosts, lipoproteins, liposomes, and micelles. The carriers can be made slowly degradable, stimuli-reactive (e.g., pH- or temperature-sensitive), and even targeted (e.g., by conjugating them with specific antibodies against certain converted by W eb2PDFConvert.com especially if the drug possesses amphiphilic and/or mesogenic properties. The drugs can be physically entrapped in the core of block copolymer micelles and transported at concentrations that can exceed their intrinsic water. which allows control of the size and morphology of the micelles. Controlled drug release and subsequent biodegradation are important for developing successful formulations.com . changes in pH or temperature). researchers have appreciated the potential benefits of nanotechnology in providing vast improvements in drug delivery and drug targeting. A strategy that could allow active targeting involves the surface functionalization of drug carriers with ligands that are selectively recognized by receptors on the surface of the cells of interest. as the choice of a drug is often influenced by the way the medicine is administered. and may even influence it due to molecular interactions.1. and (v) a combined erosion /diffusion process. The mode of delivery can be the difference between a drug’s success and failure. Functionalization of block copolymers with crosslinkable groups can increase the stability of the corresponding micelles and improve their temporal control. Two major mechanisms can be distinguished for addressing the desired sites for drug release: (i) passive and (ii) active targeting.characteristic components of the area of interest). Improving delivery techniques that minimize toxicity and improve efficacy offers great potential benefits to patients.g. Targeting is the ability to direct the drug-loaded system to the site of interest. A final feature that makes amphiphilic block copolymers attractive for drug delivery applications is the fact that their chemical composition. Sustained (or continuous) release of a drug involves polymers that release the drug at a controlled rate due to diffusion out of the polymer or by degradation of the polymer over time. where degradation can occur. and opens up new markets for pharmaceutical and drug delivery companies. the contents of the hydrophobic core are effectively protected against hydrolysis and enzymatic degradation. the corona may prevent recognition by the reticuloendothelial system and therefore preliminary elimination of the micelles from the bloodstream. (iii) diffusion (in the case of nanocapsules) through the carrier wall. Pulsatile release is often the preferred method of drug delivery. ADMISSION ADMISSION Figure: 1 Pharmaceutical carriers a) MICELLES: Micelles formed by self-assembly of amphiphilic block copolymers (5-50 nm) in aqueous solutions are of great interest for drug delivery applications. It is achieved by using drug-carrying polymers that respond to specific stimuli (e. When developing these formulations. (iv) carrier matrix erosion. Substitution of block copolymer ADMISSION converted by W eb2PDFConvert. or on finding alternative and acceptable routes for the delivery of protein drugs other than via the gastro-intestinal tract. as it closely mimics the way by which the body naturally produces hormones such as insulin. the goal is to obtain systems with optimized drug loading and release properties. such as the blood brain barrier. total molecular weight and block length ratios can be easily changed. The incorporated drug participates in the microstructure of the system. the hydrophilic blocks can form hydrogen bonds with the aqueous surroundings and form a tight shell around the micellar core..solubility. Potential release mechanisms involve: (i) desorption of surface-bound /adsorbed drugs. (ii) diffusion through the carrier matrix. In addition. this could allow a more precise targeting of the site of interest. ► As a Novel ► Up System ► Drug Fact ► Earth Novel For over 20 years. 1. Since ligand–receptor interactions can be highly selective. As a result. Other approaches to drug delivery are focused on crossing particular physical barriers. exposure to light. Moreover. as well as nanoparticle dispersions consisting of small particles of 10–400 nm diameter show great promise as drug delivery systems.1 Drug Delivery Carriers Colloidal drug carrier systems such as micellar solutions. vesicle and liquid crystal dispersions. in order to better target the drug and improve its effectiveness. An example of passive targeting is the preferential accumulation of chemotherapeutic agents in solid tumors as a result of the enhanced vascular permeability of tumor tissues compared with healthy tissue. long shelf-life and low toxicity. nutrients and antibiotics. while their stability and protection from the Mononuclear Phagocyte System (MPS) is being achieved by functionalization of the dendrimers with polyethylene glycol chains (PEG). POPULAR ARTICLES Figure: 2 Block copolymer micelles. They can be made to form different FO RM U LA TIO N A N D EV A LU A TIO N O F A M O XIC ILLIN TRIH YD RA TE M O D IFIED RELEA SE D O SA GE FO RM S C O M PA RA TIV E D ISSO LU TIO N STU D IES FO R A C EC LO FEN A C M A RKETED D O SA GE FO RM S REGISTRA TIO N D O SSIER O F PH A RM A C EU TIC A LS converted by W eb2PDFConvert. highly branched and monodisperse macromolecules with symmetrical architecture. The polar character of the liposomal core enables polar drug molecules to be encapsulated. determine the environment of the nanocavities and consequently their solubilizing properties.com . Targeting effectiveness is affected by attaching targeting ligands at the external surface of dendrimers. however. only allowing passive diffusion of small solutes such as ions.e. b) LIPOSOMES: Liposomes are a form of vesicles that consist either of many. PYRRO LE. driven by the concentration difference between the interior and the exterior of the nanocage. a lamellar phase) where aqueous drug solutions can be included. FU RA N . drugs that are encapsulated in a nanocage-functionalized with channel proteins are effectively protected from premature degradation by proteolytic enzymes. They consist of a central core.LTYRO SIN E D ERIV A TIV ES W ITH A N TI. The drug molecule.V ITRO EV A LU A TIO N O F H YD RO PH ILLIC M A TRIX BA SED SA LBU TA M O L SU LPH A TE TA BLETS M O LEC U LA R D O C KIN G STU D IES O F N . branching units and terminal functional groups. Participation of nonionic surfactants instead of phospholipids in the bilayer formation results in niosomes. They can be made to form different geometries. with alternative polar and non-polar layers (i. d) LIQUID CRYSTALS: Liquid Crystals combine the properties of both liquid and solid states.micelles with specific ligands is a very promising strategy to a broader range of sites of activity with a much higher selectivity. TH IO PH EN E D ERIV A TIV ES & PH A RM A C O LO GIC A L A C TIV ITIES: A REV IEW Rev iew o n: TH E PH A RM A C EU TIC A L PA C KA GIN G M A N U FA C TU RIN G D O C U M EN TA TIO N IN PH A RM A C EU TIC A L IN D U STRYD EV ELO PM EN T A N D IM PLEM EN TA TIO N FO RM U LA TIO N D EV ELO PM EN T A N D IN ..(2BEN Z O YLPH EN YL). d) LIQUID CRYSTALS: Liquid Crystals combine the properties of both liquid and solid states. Amphiphilic and lipophilic molecules are solubilized within the phospholipid bilayer according to their affinity towards the phospholipids. whereas the external groups the solubility and chemical behaviour of these polymers. Thus. is able to diffuse through the channel. few or just one phospholipid bilayers. Channel proteins can be incorporated without loss of their activity within the hydrophobic domain of vesicle membranes.D IA BETIC A C TIV ITY O F TYPE 2 D IA BETES REV IEW O N O C U LA R D RU G D ELIV ERY Figure: 3 Drug encapsulation in liposomes c) DENDRIMERS: Dendrimers are nanometer-sized. The core together with the internal units. acting as a size-selective filter. e) NANOPARTICLES: Nanoparticles (including nanospheres and nanocapsules of size 10-200 nm) are in the solid state and are either amorphous or crystalline... H erbal C o s m etic s : A s afe and effec tiv e appro ac h FO RM U LA TIO N A N D EV A LU A TIO N O F A TA Z A N A V IR SU LPH A TE FLO A TIN G M A TRIX TA BLETS A REV IEW A RIC LE O N SYN TH ESIS A N D BIO LO GIC A L PRO PERTY O F SO M E N O V EL BU TEN O LID E D ERIV A TIV ES SUBMIT YOUR ARTICLE/PROJECT AT articles@pharmatutor. Nanoparticles as drug carriers can be formed from both biodegradable polymers and non-biodegradable polymers.org A ntim ic ro bial A c tiv ity o f Plants Belo ng to So lanac eae Fam ily Subscribe to Pharmatutor Alerts by Email FIND OUT MORE ARTICLES AT OUR DATABASE 1 2 3 4 ► Earth Novel 5 6 7 ► New Cell 8 nex t › REC EN T A D V A N C E IN PU LSA TILE D RU G D ELIV ERY SYSTEM las t » SU RFA C TA N TS A N D ITS A PPLIC A TIO N IN PH A RM A C EU TIC A LS: A N O V ERV IEW ► Cancer Cell ► New Tablets Login or register to post comments T a gs Articles Pharmaceutics Articles Roorkee Uttarakhand Searc h Pharm aTuto r FIND MORE ARTICLES W O N D ERS O F IM M U N E SYSTEM : SPO N TA N EO U S REGRESSIO N O F C A N C ERS A REV IEW O N D YSLEXIA C LIN IC A L PH A RM A C Y IN IN D IA : REC EN T A D V A N C ES A N D PERSPEC TIV E C H ILD H O O D O BESITY: REA SO N BEH IN D TH IS H EA LTH C RISIS SYSTEM A TIC A PPRO A C H FO R C O M PLA IN T H A N D LIN G IN PH A RM A C EU TIC A L IN D U STRIES. while nanospheres are matrix systems in which the drug is physically and uniformly dispersed.geometries. Nanocapsules are vesicular systems in which the drug is confined to a cavity surrounded by a unique polymer membrane. converted by W eb2PDFConvert. P ha r m a T uto r E d u La b s Search For. They are able to adsorb and/or encapsulate a drug. as carriers of DNA in gene therapy.. NOW YOU CAN ALSO PUBLISH YOUR ARTICLE ONLINE. In recent years. thus protecting it against chemical and enzymatic degradation.com . a lamellar phase) where aqueous drug solutions can be included. with alternative polar and non-polar layers (i..e.. in targeting particular organs / tissues.A N U PD A TED REV IEW C H RO N O PH A RM A C O TH ERA PY O F H YPERTEN SIO N : TIM E. Like This Page TOP ARTICLES Loading NEWS. biodegradable polymeric nanoparticles have attracted considerable attention as potential drug delivery devices in view of their applications in the controlled release of drugs.D EPEN D EN T EFFEC TS O F TREA TM EN T O N BLO O D PRESSU RE A C A SE STU D Y O N H EM O LYTIC U REM IC SYN D RO M E.LEA D IN G TO A C U TE REN A L FA ILU RE TA RGETED D RU G D ELIV ERY SYSTEM S FO R LU N G C A N C ER N EED A N D A PPLIC A TIO N O F A N A LYTIC A L M ETH O D D EV ELO PM EN T O N N EW FIXED D O SE C O M BIN A TIO N O F IRBESA RTA N A N D A TO RV A STA TIN IN PH A RM A C EU TIC A L IN D U STRY REV IEW : PLA GIA RISM A N A C T O F U N ETH IC S Privacy Policy | Disclaimer | Terms of Use | Advertise | Sitemap | Send Feedback C o p y r ight © 2 0 0 8 .2 0 1 5 . and in their ability to deliver proteins. peptides and genes through the peroral route.