This document discusses protein and peptide delivery as a novel drug delivery system. It covers the structures of proteins, advantages of protein and peptide drugs like insulin, barriers to delivery like enzymatic and epithelial barriers, and various formulation strategies to overcome these barriers. These include protein sequence modification, microencapsulation, PEGylation to increase half-life, and formulating proteins with permeabilizers. The successful delivery of protein and peptide pharmaceuticals will rely on overcoming biological membrane barriers and these drugs may replace many existing drugs.

1. PROTEIN AND PEPTIDE DELIVERY
GOEL INSTITUTE OF PHARMACY
AND SCIENCES LUCKNOW
Under the Guidance of
Mrs. Monika Joshi
Prepared by
Aditya Chaudhary
M.Pharm 1st year
(Pharmaceutics)

2. Contents
 Introduction
 Structure Of Protein
 Advantages Of Protein And Peptide Delivery
 Disadvantages Of Protein And Peptide Delivery
 Barriers To Protein And Peptide Delivery
a) Enzymatic Barrier
b) Intestinal Epithelial Barrier

3. Contents
c) Capillary Endothelial Barrier
d) Blood Brain Barrier
 Delivery Of Protein And Peptide Drugs
 Formulation Of Protein And Peptide Delivery
 Conclusions

4. Introduction
➢ Protein and peptide delivery are the Novel
Drug Delivery System. They are abundantly
available in biological cells.
➢ They act as hormones, structural elements and
immunoglobins etc.
➢ The accumulation of amino acids forms peptide
and accumulation of peptide form protein.
➢ Absence of protein and peptide cause disease
Diabetes Mellitus.

5. Structures Of Protein
1. Primary Structure: Array of number and
sequence of sequence of amino acids in
protein Structure.
2. Secondary Structure : Regularly repeating
local structures stabilized by hydrogen
bond.
3. Tertiary Structure: There dimensional
Structure of functional protein.
4. Quaternary Structure : Contains two or
more polypeptide chains associated by
non- covalent forces.

6. Advantages Of Protein And
Peptides Delivery
 Erythroprotein is mainly used for production of
RBC.
 The protein tissue plasminogen activator is
used for Heart attack, stroke.
 Oxytocin is used in management of labor pain.
 Brandywine increases the peripheral
circulation.
 Somatostatin decrease bleeding in gastric ulcer.
 Insulin maintain blood sugar level.

7. Disadvantages Of Protein
And Peptides Delivery
 Short biological half life.
 Very large and unstable molecules.
 Structure is held together by weak non –
covalent bond forces.
 Early destroyed by relatively mild storage
conditions and gastric juices.
 Hard to obtain in large quantities.

8. Barriers To Peptide And
Protein Delivery
The successful delivery of peptide and protein-based
pharmaceuticals is primarily determined by its ability
to cross the various barriers presented to it in the
biological membrane.
There are various barriers are :
 Enzymatic Barriers
 Intestinal Epithelial Barriers
 Capillary Endothelial Barrier
 Blood Brain Barrier (BBB)

9. Delivery Of Protein And
Peptide Drugs
Different routes including –
1. Oral route
2. Buccal route
3. Nasal route
4. Transdermal route
5. Pulmonary route
6. Rectal route
7. Parentral route

10. Formulation Of Protein
And Peptide Delivery
1
• Protein sequence modification
• PEGylation
2
• Proteinylation
• Microsphere encapsulation
3
• Formulating with permeabilizer

11. Protein Sequence Modification
 The practical process of determining the
amino acid sequence of all part of protein and
peptide and moulding it as per the requirement.
 They are also called as Site directed
mutagenesis.

12. PEGylation
 The modification of biological molecules by
covalent conjugation with polyethylene glycol
(PEG), non- toxic, nonimmunogenic
polymer.
 And it is used as a strategy to overcome
disadvantages associated with some
biopharmaceiuticals.

13. PEGylation

14. Proteinylation
 The modified peptide from the desired proteins
means the attachment of additional or secondary (non
- immunogenic) proteins for in vivo protection.
 Cross – linking with Serum Albumin.
 Increase in vivo half life.
 Cross – linking or connecting by protein engineering
with antibody fragements.
 A loosely bound aggregation of several peptides
forming a colloidal particle or protein called Peptide
Micelles

15. Proteinylation

16. Conclusion
 Protein and peptide based pharmaceuticals are
rapidly becoming a very important class of
therapeutic agents and are likely to replace
many existing organic based pharmaceuticals
in the very near future.
 These drugs will be produced on a large scale
by biotechnology processes and will become
commercially available for therapeutic use.

17. Refrences
❖ Drug Stability Principles and practices By
J.Carstensen, Stability of Polypeptides and
Proteins Page no: 560-572.
❖ Advances in Controlled and Novel Drug Delivery
By N.K. Jain, Oral Delivery Of protein and
peptides Page no: 232-235.

18. THANK YOU !!