Drug Release Agents

          ABSRACT

The purpose of this research work was to examine drug release agents and the several delivery systems for which both natural and synthetic polymers have been employed for their design and fabrications. Under these facts, a large number of delivery systems made from synthetic polymer materials were found to be non-biodegradable, non-biocompatible and thus tend to impose both adverse mechanical and physiological effects on man when consumed especially on respiratory process. Whereas, delivery agents composed of natural polymeric materials such as chitosan, cellulose, alginate, starch, dextrin, gelatin, etc were reported by several literatures to be biodegradable and also compatible with the human biological system. Base on these desirable physiological properties found to be exhibit by natural polymer base delivery agents, chitosan being one of the primary natural base polymeric materials was produced from its source; chitin (exoskeleton of crustacean e.g. shrimps) and some physico-chemical properties that made possible the functional requirement of chitosan as a drug release agent were measured and determined. The molecular weight (MW) of the chitosan produced was found to be 2.889 × 106 gmol-1  with reduced viscosity ranging from 28.580 to 29.150 (mLg-1 × 102). The intrinsic viscosity obtained as the intersect of the Hypgin’s equation was 28.46 (mLg-1 × 102). Swelling index (SI) of the chitosan in hydrocarbon solvents (benzene, toluene and n-hexane) was in the range of 116.25±8.00% to 186.25±7.465%. The fat and water binding capacity (FBC & WBC) were found to be 384.76% and 542% respectively. The chitosan was converted to TPP-chitosan and chitosan hydrochloride by chemical modification with STPP and hydrochloric acid. The FBC and WBC of the TPP-chitosan were 463.75±4.17% and 639.50±9.03% and its swelling index in hydrocarbon solvents range from 190±10.8% to 258.75±8.26%.The swelling index of the chitosan hydrochloride in hydrocarbon was found to be in the range of 180.75±2.428% to 192.75±2.287%.

TABLE OF CONTENT 

Abstract                        

CHAPTER ONE 

1.0.0.  Background of the study              

1.1.0.  The delivery Quartet                 

1.2.0.  Anatomical, physiological and biochemical consideration.    

1.3.0.  Specialised Drug Delivery Systems.          

1.3.1. Osmotic Pump Device (Oros)                 

1.3.2. Floating Dosage Form (FDF)                  

1.3.3. Mucoadhesive Dosage System (MADS)            

1.3.4. Ocular Inserts                  

1.3.5. Transdernal Patches                    

1.3.6. Transnasal system                 

1.4.0.  Targeted site Specific Delivery system.           

1.4.1. Prodrug.                     

1.4.2. Natural or Passive Targeting.               

1.4.3. Active or Ligard mediated Targeting.            

1.4.4. External or Extracorperal guidance systems.         

1.4.5. Per oral Delivery Systems for Therapeutic protein and peptides

1.4.6. Micro-encapsulation technology            

1.5.0. Objectives                  

1.6.0.  Aims                    

1.7.0.  Literature Review                

1.7.1. Swelling Agents                  

1.7.2. Swelling Process                  

1.7.3. Swelling  Mechanism                

1.7.4. Investigated passed Work Report            

1.7.5. Isotropic swelling                 

1.7.6. Pharmaceutical Application of Swellable hydrogels      

1.7.7. Super Disintegrants               

1.8.0.  Scope of studies.               

1.8.1. Hydrogels and their Preparation.            

1.8.2.  Types of hydrogels.               

1.8.3. pH Sensitive hydrgels.              

1.8.4. Thermosensitive hydrogels.              

1.8.5. Polymer Blend.                

viii  1.8.6. Electrical sensitive Hydrogels.              

1.8.7. Enzyme Sensitive Hydrogels              

1.9.0.  Preparation of hydrogels              

1.9.1. Solution polymerisation/cross linking           

1.9.2. Suspension polymerisation.            

1.9.3. Polymerisation by Irridiation.             

1.9.4. Chemically cross Linked Hydrogel.          

1.9.5. Physically Cross Linking Hydrogels.            

1.10.0.  Standard methods for Hydrogels preparation.        

1.10.1.  Synthesis of hydrogels from monomers.        

1.10.2.  Synthesis of hydrogels from Prepolymers.        

1.10.3.  Synthesis of hydrogels from Polymers.                

1.10.4.  Gelation-Base hydrogels.             

1.11.0.  Research Justification.              

1.11.1.  Relevance of Chitosan.             

1.11.2.  Preparation of Chitosan Hydrogel          

1.11.3.  Material collection/Preparation.           

1.11.4.  Cross Linking of Chitosan. 

           

CHAPTER TWO 2.0.0. Methodology.                  

2.1.0. Materials and reagents.              

2.1.1. Material Collection.                

2.1.2. Reagents Used

2.1.3. Apparatus Used                 

2.2.0. Preparation of Material.                

2.3.0. Reagents Preparation.                

2.4.0. Production of Chitin.               

2.4.1.Demineralisation.                  

2.4.2. Deproteinisation.                  

2.4.3. Decolourisation.                 

2.4.4. Production of Chitosan (Deacetylation of Chitin)        

2.4.5. Preparation of Cross-Linked Chitosan  Hydrogel (TPP-Chitosan).  

2.4.6. Preparation of Chitosan hydrochloride.          

2.5.0. Determination of Physicochemical and Functional Properties.    

2.5.1. Yield.                     

2.5.2. Moisture content (MC).                

2.5.3. Fat and Water Binding Capacity (FBC/WBC).        

2.5.4. Swelling properties.                

2.5.5. Flow Properties (Viscosity and Molecular Weigth).       

2.5.7. Molecular Weigth Determination and Degree of Polymerisation.  

CHAPTER THREE 

3.0.0. Results and Discussion.               

3.1.0. Yield.                     

3.2.0. Moisture content (MC).               

3.3.0. Properties of chitosan and TPP-Chitosan.         

3.3.1. solubility Properties.                

3.3.2. Determination of FBC and WBC.            

3.3.3. Determination of Swelling index (SI).           

3.4.1. Viscosity Measurement.                

3.4.2. Molecular Weight (MW) determination and degree of polymerisation DP). 

3.5.0. Experimental Data and Results.             

CHAPTER FOUR 4.1.0. Recommendation.                  

4.2.0. Conclusion.                    

References