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PROTEIN AND PEPTIDE DELIVERY BY NASAL ROUTE: 

PRESENTED BY: GUIDED BY: RAJ BHATT MRS.VIDYA SABLE DEPT OF PHARMACEUTICS BARODA COLLEGE OF PHARMACY, LIMDA PROTEIN AND PEPTIDE DELIVERY BY NASAL ROUTE

PRESENTATION OUTLINE : 

PRESENTATION OUTLINE PROTIEN AND PEPTIDE MECHANISM NASAL ROUTE PROBLEMS WITH PROTIEN AND PEPTIDE CHALLENGES APPROCHES MERITS AND DEMERITS APPLICATION OF NASAL DELIVERY MARKETED PRODUCTS CONCLUSION

PROTIEN AND PEPTIDE: 

PROTIEN AND PEPTIDE Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. Peptides are short chains of amino acids. Peptides are frequently created by the digestion of proteins in the body. Many peptides work as hormones, neurotransmitters and as natural pain relievers.

MECHANISM: 

MECHANISM Fig 2 (A1) Intercellular spaces, (A2) Tight junctions, (B1) Passive diffusion, (B2) Active transport, (C) Transcytosis

NASAL ROUTE: 

NASAL ROUTE EXPLOITED TO PRODUCE LOCAL ACTION ON MUCOSA A PROMISING OPTION FOR PROTEIN DELIVERY FIRSTLY IN TWENTIES OXYTOXIN & INSULIN WERE TRIED THRO’ THIS ROUTE FOR SYSSTEMIC DELIVERY MOST EFFECTIVE ONE AFTER PARENTERAL ROUTE

DIMENSIONS: 

DIMENSIONS LENGTH IS 12 CMS VOLUME IS 15 ML THICKNESS OF MEMBRANE IS 3 MM AREA IS 150 CM 2

PROBLEMS WITH PROTIEN AND PEPTIDE: 

PROBLEMS WITH PROTIEN AND PEPTIDE PHYSICAL INSTABILITY 1. Denaturation : 2. Adsorption: 3. Aggreation & Precipitation

CHEMICAL INSTABILITY : 

CHEMICAL INSTABILITY Oxidation & Reduction Proteolysis Disulphide exchange Racemization Deamidation

BIOLOGICAL INSTABILITY : 

BIOLOGICAL INSTABILITY Enzymatic barrier: Intestinal epithelial barriers

PowerPoint Presentation: 

Factors Influencing Nasal Drug Absorption: Molecular Weight Enzymatic Degradation Environmental pH

CHALLENGES : 

CHALLENGES Improve physiochemical properties of drug & formulation Increase drug permeability & dissolution Modify nasal membrane Enhance drug residence time Reduce drug affinity to nasal enzymes Inhibit nasal enzymes Protect drug from nasal enzymes Reduced the rapid mucociliary clearance

APPROACHES : 

APPROACHES Prodrugs Co-Solvents Enzymatic inhibitors Permeation enhancers Formulation approach Mucoadhesion

MERITS : 

MERITS BETTER DRUG ABSORPTION DUE TO HIGH VASCULARISATION BYPASSES FIRST PASS METABOLISM FAST ON SET OF ACTION CONVINIENT, SIMPLE AND PRACTICAL WAY OF DRUG ADMINISTRATION FOR PAEDRIATRICS , GERIATRICS AND BLIND PATIENTS

DEMERITS: 

DEMERITS DISEASED STATES LIKE ALLERGIC RINITIS INFLUENZA MAY CHANGE THE NASALENVIRONMENT LONG TERM USE MAY LEAD TO TOXICITY OF CILIA AND MUCOSA

APPLICATION OF NASAL DELIVERY: 

APPLICATION OF NASAL DELIVERY 1. Treatment of epilepsy and schizophrenia: 2. Treatment of migraine 3. As an antidepressant 4. Treatment of angina pectoris and neurological deficit 5. Treatment of amnesia 6. Intranasal delivery of peptides 7. Intranasal delivery of vaccine 8. Intranasal delivery of analgesics

Marketed products : 

Marketed products Peptide/protein M wt. Formulation Company/stage Desmopressin 1,183 Solution Aventis, Ferring Salmon calcitonin 3,432 Solution Novartis,Aventis Nafarelin 1,322 Solution Pfizer \Oxytocin 1,007 Solution Novartis Buserelin 1,300 Solution Aventis

CONCLUSION : 

CONCLUSION The nasal mucosa offers several advantages for controlled drug delivery. The mucosa is well supplied with both vascular and lymphatic drainage; first-pass metabolism in the liver and presystemic elimination in the GI tract is avoided. Nasal drug delivery is a promising area for systemic delivery of orally inefficient drugs as well as an attractive alternative for noninvasive delivery of potent peptide and perhaps protein drug molecules.

REFERENCES: 

REFERENCES DRUG DEVELOPMENT & DELIVERY,ISSUE DATE, VOL 2 JUNE 4,2002 PUBMED.GOV,THE NASAL DELIVERY OF PEPTIDE AND PROTIENS,TREDS BIOTECHNOLOGY.1991AUG9(8):284-9. CONTROLLED DRUG DELIVERY CONCEPTS AND ADVANCES,BY S.P Vyas and Roop K Khar