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superporus hydrogel

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superporus hydrogel …

superporus hydrogel


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  • 1. Presented By: SANTOSH THORAT (PE/2012/315) Dept. Of Pharmaceutics12/4/2012 SUPERPORUS HYDROGEL 1
  • 2. CONTENTS Introduction Formulation Synthetic steps Generations of SPHs SPH characterization Applications Conclusions References 12/4/2012 SUPERPORUS HYDROGEL 2
  • 3. HYDROGELS:Three-dimensional networks of hydrophilic polymerchains that do not dissolve but can swell in water.both solid like and liquid like propertieshigh biocompatibilityenvironmental stimuli respondent (temperature, pH, light, specific molecules)Ideal for controlled drug deliveryClassification: Based upon PorosityI. NonporousII. MicroporousIII. MacroporousIV. Superporous 12/4/2012 SUPERPORUS HYDROGEL 3
  • 4. Superporous hydrogels (SPHs) The fast swelling property is based on water absorption through open porous structure by capillary force. SWELLING PROPERTIES : The SPHs swell immediately upon contact with water regardless of their size in the dried state. The SPHs unique property of size independent fast swelling kinetics of SPHs is accounted for by their interconnected open cellular structure The open porous structure allows extremely fast absorption of water into the center of the dried matrix by capillary force 12/4/2012 SUPERPORUS HYDROGEL 4
  • 5. Formulations for SPHMaterial RoleAcrylamide, Acrylic acid MonomerBisacylamide Cross-linkerDeionized water SolventAmmonium persulfate OxidantTetramethyl ethylenediamine ReductantGlacial acetic acid Foaming aidSodium bicarbonate Foaming agentPEO–PPO–PEO block copolymers Foam stabilizerH. Omidian et al. / Journal of Controlled Release 102 (2005) 3–12 12/4/2012 SUPERPORUS HYDROGEL 5
  • 6. Synthetic steps:  Step 1: The monomer is first diluted with certain amount of water to reach a desired monomer concentration.  Step 2: Dilution with water also makes it easy to handle the monomers. For instance, the water-diluted glacial acrylic acid possesses superior handling properties as compared with acrylic acid because of its lower freezing temperature.  Step 3 Addition of a cross-linker.  Step 4: To produce a foam during polymerization , foaming aid such as glacial acetic acid and acrylic acid are added to the monomer solution. 12/4/2012 SUPERPORUS HYDROGEL 6
  • 7.  Steps 5: To promote polymerization, redox couples of ammonium persulfate / sodium metabisulfite or potassium persulfate /sodium metabisulfite and thermal initiators, such as ammonium persulfate or potassium persulfate , are used. Steps 6 : Since the foam stability is essential for producing homogeneous SPHs, surfactants, such as PEO–PPO–PEO triblock copolymers, are used during the synthesis. Step 7 : Lastly, to generate gas bubbles, acid- dependent foaming agent, such as sodium bicarbonate is added to the formulation. 12/4/2012 SUPERPORUS HYDROGEL 7
  • 8. Postsynthesis steps of SPHs. Dehydration using ethanol: helps to stabilize the foamed product and prevent it from shrinking. Drying 12/4/2012 SUPERPORUS HYDROGEL 8
  • 9. Generations of SPHs The first-generation SPHs: Conventional SPHs Characterized by fast swelling, High swelling ratio, Weak mechanical properties. The second-generation SPHs: SPH composites Characterized by fast swelling, Medium swelling ratio Improved mechanical properties. The third-generation SPHs: SPH hybrids possess elastic properties that can be highly useful in the development of gastrointestinal devices 12/4/2012 SUPERPORUS HYDROGEL 9
  • 10. Structural, swelling and mechanicalproperties of various SPH generations  H. Omidian et al. / Journal of Controlled Release 102 (2005) 3–12 12/4/2012 SUPERPORUS HYDROGEL 10
  • 11. 12/4/2012 SUPERPORUS HYDROGEL 11
  • 12. The first-generation SPHs: Conventional SPHs In 1999, Chen et al prepared SPHs with fast swelling kinetics and superabsorbent properties for the first time. The dried SPHs swell fast to a large size, larger than a few hundred times. Difficult to handle without breaking. The CSPHs are fragile against bending or tensile stresses. The lack of desirable mechanical properties of the conventional SPHs triggered the development of the second-generation SPH composites. Hossein Omidian et al,JPP 2007, 59: 317–327 12/4/2012 SUPERPORUS HYDROGEL 12
  • 13. The second-generation SPHs:SPH composites A matrix-swelling additive or a composite agent is utilized. As the cross-linking polymerization proceeds throughout the solution, individual swollen composite agent particles are connected together through polymer chains connecting them. The presence of composite agent in SPH composites results in improved mechanical properties over conventional 12/4/2012 SUPERPORUS HYDROGEL 13
  • 14. The third-generation SPHs: SPH hybrids a water-soluble counterpart (hybrid agent e.g. Sodium alginate, sodium carboxymethyl cellulose and chitosan) is employed with the third generation SPH formulations. Integrated semi-interpenetrating network will be formed first. Ethylenebisacrylamide has been utilized as a thermally resistant chemical crosslinker. 12/4/2012 SUPERPORUS HYDROGEL 14
  • 15. SPH characterization Surface Morphology: SEM Porosity: Mercury porositometer. Thermal properties: 13C nuclear magnetic resonance (NMR) and differential scanning calorimetry (DSC). 12/4/2012 SUPERPORUS HYDROGEL 15
  • 16.  Swelling: swelling and mechanical properties are generally sensitive to the type and nature of the swelling medium (Ionic strength,pH, salts, organic solvents and pressure). Where, Ms and Md are the weight of the hydrogel in the swollen and dried states Measured gravimetrically and volumetrically swelling parameters can be evaluated at low (room temperature) or medium/ high temperatures (body fluid temperature of 37°C) Tcore -The Tcore identifies the opaque/transparent transition in SPHs. 12/4/2012 SUPERPORUS HYDROGEL 16
  • 17.  Mechanical properties: Regular mechanical testers and texture analysers are commonly used to evaluate SPH mechanical properties. 12/4/2012 SUPERPORUS HYDROGEL 17
  • 18.  Gastric simulator: The simulator measures the amount of energy absorbed by the sample until it fails under certain stresses 12/4/2012 SUPERPORUS HYDROGEL 18
  • 19.  Safety/toxicity: Clinical observations, clinical pathology, chemistry and haematology, ethylene glycol and glycolic acid were monitored during this study. Induction of emesis within approximately 45min to 2 h post-dose did not cause any safety concerns such as oesophageal obstruction 12/4/2012 SUPERPORUS HYDROGEL 19
  • 20. PHARMACEUTICAL APPLICATIONS1. Development of gastric retention devices2. Development of fast-dissolving tablets3. Development of diet aid4. SPH-based gastroretentive platforms5. Chemoembolization and occlusion devices 12/4/2012 SUPERPORUS HYDROGEL 20
  • 21.  DEVELOPMENT OF GASTRIC RETENTION DEVICES The idea was to make an oral formulation to swell fast to a size large enough to prevent them from passing through the pylorus. Maximum swelling should in about 20 minutes because water is known to remain in the stomach for about 30 minutes e.g. Superporous Hydrogels for Metoprolol Tartrate as a Gastro Retentive System 12/4/2012 SUPERPORUS HYDROGEL 21
  • 22.  DEVELOPMENT OF PERORAL PEPTIDE DELIVERY SYSTEMS Superporous hydrogels and their composites that increase their volume by about 200-fold. Such volume increase allowed the gels to mechanically stick to the intestinal gut wall and deliver the incorporated drug directly to the gut wall. e.g. buserelin, octreotide and insulin 12/4/2012 SUPERPORUS HYDROGEL 22
  • 23.  DEVELOPMENT OF FAST DISSOLVING - TABLETS By the direct compression method is to add fine particles of superporous hydrogels to the drug and other excipients. Superporous hydrogel microparticles possess open pore structures This unique porous structure allows for transport of water through capillary forces. Yang et al (2004) used poly (acrylic acid)-based SPH microparticles to make fast-melting tablets of ketoprofen. The tablets could swell to about 80 and 50 times in distilled water and 0.2 M phosphate buffer, respectively. 12/4/2012 SUPERPORUS HYDROGEL 23
  • 24.  DEVELOPMENT OF DIET AID Superporous hydrogel tablets so that the swollen superporous hydrogels can occupy a significant portion of the stomach space, leaving less space for food. The presence of a bulky gel or gels in the stomach is expected to suppress the appetite. 12/4/2012 SUPERPORUS HYDROGEL 24
  • 25.  SPH-BASED GASTRORETENTIVE PLATFORMS Requirements for a swellable gastroretentive platform were found to be swelling rate (within minutes), swelling capacity (preferably 8– 15% v/v), shape, mechanical strength (resist pressures in the range 0.5–2.0 N cm−2, preferably in the fed state), flexibility, a controlled disintegration, ease of drug loading, stability and pharmaceutical acceptability. 12/4/2012 SUPERPORUS HYDROGEL 25
  • 26.  CHEMOEMBOLIZATION: Embolization has been used for cancer treatment by restricting the oxygen supply to the growing tumours. A chemotherapeutic agent and an anti- angiogenic agent could be loaded into SPHs for chemoembolization therapy. They fit better in the blood vessels and provide better blocking. 12/4/2012 SUPERPORUS HYDROGEL 26
  • 27. Non-pharmaceutical Applications  Superporous hydrogels are also useful in the development of simple tools for prevention of water leakage.  They can also be used for preventing water spill around water-sensitive materials.  Superporous hydrogels are useful for making toys that can change their sizes and colors extremely fast. 12/4/2012 SUPERPORUS HYDROGEL 27
  • 28. Conclusions Superporous hydrogels are a new class of hydrogel materials that, regardless of their original size, rapidly swell to a large size. Different generations of SPHs evolved to address the needs for certain pharmaceutical applications. Various pharmaceutical and biomedical applications of superporous hydrogels have been made, and several products are under development. 12/4/2012 SUPERPORUS HYDROGEL 28
  • 29. References Hossein Omidian, Jose G. Rocca, Kinam Park,” ReviewAdvances in superporous hydrogels” Journal of Controlled Release 102 (2005) 3 –12. Assadang Polnok , J. Coos Verhoef ,Gerrit Borchard,Narong Sarisuta, Hans E. Junginger,” In vitro evaluation of intestinal absorption of desmopressin using drug-delivery systems based on superporous hydrogels” International Journal of Pharmaceutics 269 (2004) 303–310. Jia Kuang, Kun Young Yuk, Kang Moo Huh,” Polysaccharide-based superporous hydrogels with fast swelling and superabsorbent properties”, Carbohydrate Polymers 83 (2011) 284–290. Cui Tang , Chunhua Yin , Yuanying Pei , Min Zhang , Lifang Wu, ” New superporous hydrogels composites based on aqueous Carbopol solution (SPHCcs): synthesis, characterization and in vitro bioadhesive force studies”, European Polymer Journal 41 (2005) 557–562. 12/4/2012 SUPERPORUS HYDROGEL 29
  • 30.  Dukjoon Kima, Kinam Park,” Swelling and mechanical properties of superporous hydrogels of poly(acrylamide-co-acrylic acid)/polyethylenimine interpenetrating polymer networks”, Polymer 45 (2004) 189–196. Jun Chen, Kinam Park,” Synthesis and characterization of superporous hydrogel composites”, Journal of Controlled Release 65 (2000) 73–82. Hossein Omidian, Kinam Park and Jose G. Rocca,” Recent developments in superporous hydrogels” JPP 2007, 59: 317–327. N Vishal Gupta , HG Shivakumar,” Development of a Gastroretentive Drug Delivery System based on Superporous Hydrogel”, Tropical Journal of Pharmaceutical Research June 2010; 9 (3): 257-264. 12/4/2012 SUPERPORUS HYDROGEL 30
  • 31. 12/4/2012 SUPERPORUS HYDROGEL 31