Protein and Peptide.pptx

Protein and Peptide drug delivery system are the Novel drug Delivery System. Proteins and peptides are the most abundant components of biological cells. They exist functioning such as enzymes, hormones, structural element and immunoglobulin. Proteins and peptides are therefore almost exclusively administered by the parenteral route. Although parenteral administration serves the purpose, it has several shortcomings. It encounters, many barriers affecting its stability, such as poor cellular membrane permeability at the GIT site, enzymatic degradation (various proteases), and first-pass hepatic metabolism.

1. DRUG DELIVERY SYSTEM M. PHARM PHARMACEUTICS PROTEIN AND PEPTIDE DRUG DELIVERY SUBMITTED BY: RAHUL PAL M. PHARM SUBMITTED TO: MR. GULSHAN RATHORE DEPARTMENT OF

2. PROTEIN & PEPTIDE PROTEINS : Proteins are the large organic compounds made of amino acids arranged in a linear chain and joined together by peptide bonds. Protein > 50 amino acids PEPTIDES : These are short polymers formed from the linking, in a defined order of amino acids. Peptide < 50 amino acids

3. Transport and storage of small molecules. Coordinated motion via muscle contraction. Mechanical support from fibrous protein. Generation and transmission of nerve impulses. Enzymatic catalysis. Immune protection through antibodies. Control of growth and differentiation via hormones FUNCTIONS OF PROTEINS

4. Erythropoietin used for production of RBC . Tissue plasminogen activator is used for Heart attack, Stroke. Oxytocin maintain labor pain ( caused by contractions of the muscles of the uterus and by pressure on the cervix) . Bradykinin increases the peripheral circulation. Somatostatin decrease bleeding in gastric ulcer. Gonadotropin induce ovulation. Insulin maintain blood sugar level. IMPORTANCE OF PROTEINS

5. Enzymatic B arrier : L imits absorption of protein drugs fr om G.I. tract. Intestinal Epithelial Barrier involved in the transport of protein drugs across the intestinal epithelium. Capillary E ndothelial B arrier involved in transport of protein drugs across the capillary endothelium. Blood Brain B arrier (BBB). BARRIERS TO PROTEIN DRUG DELIVRY

6. The oral delivery of therapeutic proteins and peptides can be successfully, Achieved by using various carrier systems like: Dry Emulsions (Dry emulsions are prepared by drying liquid o/w emulsions containing a solid carrier in the aqueous phase) Cellular Carriers (e.g.: Resealed erythrocytes) Microspheres, Liposome, Nanoparticles . Hydrogels (drugs enclosed in gelling polymers) FORMULATION OF DELIVERY SYSTEM

7. There are of four types of protein: Primary Protein- T he amino acid sequence. Secondary Protein : Regularly repeating local structures stabilized by hydrogen bond. Tertiary Protein : Three dimensional (3D) structure of polypeptide. Quaternary Protein : The structure formed by several protein molecules (polypeptide chain). STRUCTURE OF PROTEIN

8. DIFFERENT PROTEIN STRUCTURES

9. Why we need Protein and Peptide Drug? The protein and peptide are very important in biological cells. Lack of protein and peptide causes disease like Diabetes Mellites (DM). Diabetes Mellitus (DM) is caused by the lack if protein called Insulin . Now a days R-DNA technology and hybridoma technique also used in protein and peptide based pharmaceuticals.

10. Stability Testing : The capability of a particular formulations in a specific container/closure system to remain within its physical, chemical, microbiological, toxicological and protective specification. Evaluate the effect of environmental factors on the quality of the drug substance or a formulated product which is utilized for prediction or its shelf life and proper storage condition. EVALUATION OF PROTEIN AND PEPTIDE DELIVERY

11. Due to complexity of protein, bioassay are required to asses potency of the formulation. Bioassay are two types: in vitro and in vivo. In case of in vitro bioassay response of cells to hormones and growth factors is monitored. In case of in vivo bioassay pharmacological response of animals to protein s monitored. E.g. Post injection BSL in rabbits is measured for bioassay of insulin. BIOASSAY

12. Protein containing aromatic amino acid residues such as phenyl alanine, tyrosine, tryptophan can be detected by UV Spectroscopy. It can be used as an analytical determination methods. In the presence of protein in an acidic medium, absorption maximum of Coomassie brilliant blue G-250 dye changes. Lastly the determination of concentration of the protein in the sample. UV Spectroscopy Bradford Assay

13. DSC used as a tool for investigating transition of conformation as a function of temperature and more important, the effect of potential stabilizing excipients in a protein solution. Used to study stability of protein and peptide. Various modes used are: Normal Phase HPLC Reverse Phase HPLC Ion exchange Chromatofocusing. Chromatography Differential Scanning Calorimetry Electrophoresis

14. Smart Polymer based delivery system: Biodegradable polymeric systems delivering protein and peptide drugs. Smart polymer-based injectable drug delivery systems. Smart polymer are classified according to the external stimulus they respond to: 01. Temperature Sensitive : Poly (ethylene oxide)-poly (propylene oxide). 02. pH Sensitive Polymer : Poly (methacrylic acid). 03. Photo-Sensitive Polymer : Polyvinyl alcohol. 04. Phase Sensitive Polymers : Poly (D,L –Lactide) RECENT ADVANCE

15. Leupron : (Drug - Leuprolide : Used for Prostatic cancer) Pergonal : (FSH & LH: Used in cases of female infertility) Calcimar : (Salmon Calcitonin: Used to treat Hypercalcemia) Acthar : (Corticotrophin: Used in cases of Hormone deficiency) Certain Marketed Formulations