This document discusses protein and peptide drug delivery systems. It begins by defining proteins and peptides, and describing their structures. It then discusses the need for protein and peptide delivery systems due to their importance in biological processes. Various pharmaceutical approaches for protein and peptide delivery are described, including chemical modification, enzyme inhibitors, penetration enhancers and formulation vehicles. Finally, some examples of marketed protein and peptide formulations are provided.

1. PROTEIN AND PEPTIDE DRUG
DELIVERY SYSTEM
PRESENTED BY GUIDED BY
PRIYANKA GOSWAMI KOUSHIK SEN GUPTA
M.PHARM 2ND SEM ASSOCIATE PROFESSOR
FACULTY OF PHARMACEUTICAL SCIENCE FACULTY OF PHARMACEUTICAL SCIENCE
ASSAM DOWN TOWN UNIVERSITY ASSAM DOWN TOWN UNIVERSITY

2. CONTENT
• INTRODUCTION
• STRUCTURE OF PROTEIN
• CLASSIFICATION OF PROTEIN
• NEED OF PROTEIN AND PEPTIDE DRUG DELIVERY SYSTEM
• FUNCTION
• ADVANTAGE
• ROUTE OF ADMINISTRATION
• PHARMACEUTICAL APPROACHES
• MARKATED FORMULATION
• REFERRENCE
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3. INTRODUCTION
• Protein and peptide drug delivery system are the noval
drug delivery system .The term protein is derived from
the Greek word proteios which means “holding the first
place”.
• PROTEINS: Proteins are the high molecular weight
joined together by a peptide bond and possesses 50 or
more amino acid. Protein occur in every part of all
living cell for giving nutritional activity for providing a
body building activity.
• PEPTIDES: These are short polymers contain less then 20
amino acid and having molecular weight less then 5000
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4. STRUCTURE OF PROTEIN
• Primary structure: It is a linear sequence of amino
acid that makes up polypeptide chain
• Secondary structure: Two most common type of
secondary structure are alpha helix and beta pleated
sheet
• Tertiary structure: It is formed by bending and
twisting of the polypeptide chain.
• Quaternary structure: Two or more polypeptide
chain hold together by non-covalent bond to give the
quaternary structure of the proteins
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6. CLASSIFICTION
Depending on solubility
• Globular protein: this category of protein are soluble
in water or common salt. E.g. Ovalbumin
• Fibrous protein: this are insoluble in water and
common salt. E.g. keratins, collagens, elastin
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7. CLASSIFICTION
Depending on complexity
• Simple protein: On hydrolysis they yield only the amino
acids and occasional small carbohydrate compounds.
Examples are: albumins, globulins, glutelins,
albuminoids, histones and protamines.
• Conjugated protein: These are simple proteins combined
with some non-protein material in the body. Examples
are: nucleoproteins, glycoproteins, phosphoproteins,
haemoglobins and lecithoproteins.
• Derived protein: These are proteins derived from simple
or conjugated proteins by physical or chemical means.
Examples are: denatured proteins and peptides.
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8. NEED OF PROTEIN AND PEPTIDE
DRUG DELIVERY SYSTEM
• The protein and peptides are very important in
biological cells and organic molecules.
• In the absence of proteins and peptides causes
diseases like Diabetes mellitus.
• Now a days recombinant DNA technology and
hybridoma techniques also used in protein and
peptide based pharmaceuticals
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9. FUNCTION
• Transport and storage of small molecules and
biological molecules.
• Coordinated motion via muscle contraction.
• Generation and transmission of nerve impulses.
• Enzymatic catalysis in biochemical reactions.
• The Immune protection through antibodies.
• The Control of growth and differentiation via
hormones.
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10. ADVANTAGES
• Erythropoietin 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.
• Bradykinin increases the peripheral circulation.
• Somatostatin decrease bleeding in gastric ulcer.
• Gonadotropin induce ovulation.
• Insulin maintain blood sugar level.
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11. ROUTE OF ADMINISTRATION
• Parenteral systemic delivery
• Non‐parenteral systemic delivery
• Oral route
• Nasal route
• Buccal route
• Ocular route
• Rectal route
• Transdermal route
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12. ROUTE OF ADMINISTRATION
• Most of the pharmaceutical proteins and peptides
preparations are formulated as solution, suspension,
emulsion and they are delivered via parenteral or
non-parenteral.
• Parenteral systemic delivery: these route is the most
efficient way it consist I.V, I.M, S.C. but these routes
have its own difficulties such as poor patient
compliance, pain, discomfort and inconvenient to
treat paediatric patient.
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13. ROUTE OF ADMINISTRATION
Non‐parenteral systemic delivery
Oral route: the oral route of administration in protein and peptide is
suitable as compared to parenteral route in regard to higher patient
compliance. But the development of oral drug delivery of protein and
peptide is having several drawback such as:
Nasal route: the nasal route has been employed for producing local
action on the mucosa which is more permeable compared to oral
mucosa
Advantages:
• Rapid onset of action
• Avoid first pass metabolism.
• Better drug absorption.
Disadvantage:
• Long term usage cause toxicity
Buccal route: it is well acceptable to the patient, easy to administrate
and it is attached or removed without any pain or discomfort.
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14. ROUTE OF ADMINISTRATION
 Ocular route: the systemic bioavailability achieved by this route is
very low.
 Rectal route: This route of delivery is relatively recent idea. It
improve systemic bioavailability with co-administration of
absorption enhancer. It was recently reported that a solid
dispersion of insulin with sodium salicylate can produce a rapid
release of insulin from the suppositories achieve a significant
reduction in plasma glucose levels in normal dose.
Advantages:
• It avoids first pass metabolism
• It is suitable for drug that cause nausea/ vomiting.
Transdermal route: drug is absorbed through the skin. Controlled
administration of drug is possible through this route. It improve the
patient compliance. 14

15. PHARMACEUTICAL
APPROACHES
1. Chemical modification
2.Enzyme inhibitors
3.Penetration enhancers
4.Formulation vehicle
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16. CHEMICAL MODIFICATION
The chemical modification of protein and peptide
drug delivery system is important in order to
improve the enzymatic stability as well as
membrane permeations. This can be achieved by –
 Amino acid modification
 Hydrophobization
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17. CHEMICAL MODIFICATION
• Amino acid modification: The Amino acid modification is
important to enhance the Membrane Permeability and
Maintain the Enzymatic Stability. Desmopressin and
Deaminovasopressin are the two important analogs of
vasopressin, former involves deamination of first amino acid
and replacement of last Larginine D-arginine to give
Deaminovasopressin
• Hydrophobization: This approach helps to increase the
lipophilicity of the protein or peptide moieties. Incresing
hydrophobicity of protein and peptide by surface
modification using lipophilic moieties may increase the
stability of the protein.
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18. ENZYME INHIBITORS
The enzyme (protease) inhibitors incorporate the CO-
group to the protein and peptide moiety, result in
alteration of the environment for the enzyme and
supress the proteolytic activity.
The enzyme proteases inhibitors are divided into
four types - they are Aspartic proteases (Pepsin,
Renin), Cystinyl proteases (Papain), Serinyl proteases
(Thrombin, Trypsin) and Metallo proteases
(Carboxypeptide).
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19. PENETRATION ENHANCERS
Penetration enhancers are the one of the most important
component of protein and peptides formulation and are
responsible for the disruption of the mucosal barriers and
improve the membrane permeations of large
macromolecular substances like proteins and peptides.
The several classes of compounds are mainly used as
permeation enhancers such as surfactant (Polysorbate,
SLS, Pluronic F-68), chelating agent (EDTA), fatty acids
(Sodium carprate), mucoadhesive polymeric systems
(Thiomers, Cellulose derivatives), phospholipids (PC).
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20. FORMULATION VEHICLES
• The Protein and Peptide Drug Delivery system is
important for the Oral Delivery of Protein and Peptides
can be successfully achieved by using various carrier
systems are like
1. Dry Emulsion
2. Microspheres
3. Liposomes
4. Nanoparticles
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21. MARKATED FORMULATION
Product Formulation Routes Indication
Glucagon Glucagon I.M, I.V., S.C Hypoglycemic
Acthar Corticotropin I.M, I.V, S.C Hormone deficiency
Sandostatin Octreotide S.C. Intestinal tumour
Syntocinon Oxytocin I.M, I.V Labour induction
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22. REFERRENCE
• Bruno BJ, Miller GD, Lim CS. Basics and recent advances in
peptide and protein drug delivery. Therapeutic delivery.
2013;4(11):1443-1467. doi:10.4155/tde.13.104.
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2792531/
• Sagar kishor savale, Protein and peptide drug delivery
system, world journal of pharmacy and pharmaceutical
sciences, 5, 724-742, 2016
• https://study.com/academy/lesson/primary-structure-of-
protein-definition-lesson-quiz.html
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