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superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
superporus hydrogel
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superporus hydrogel

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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

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