Barriers of Protein and Peptide Drug Delivery

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Barriers of protein and pEptide drug delivery

SHREE SURESHDADA JAIN INSTITUTE OF PHARMACEUTICAL


EDUCATION & RESEARCH JAMNER
Roll no. 03

Presented by - Guided by –
Aashish Kishor Chaudhari Mr. Samir Shaikh Lecturer
F. Y. M Pharm (Sem- 1st) & PG Teacher
Dept. of Pharmaceutics Dept. of Pharmaceutics
~: content :~

1. Define Protein and Peptide .


2. Barriers to Protein and Peptide drug delivery .
 Enzymatic Barriers .
 Intestinal Epithelial Barriers .
 Capillary Endothelial Barriers .
 Blood Brain Barriers .
-: Define - Protein and Peptide

 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.
~: Barriers to protein drug delivery :~

1. Enzymatic barriers :-

 Major enzymatic barrier to absorption of proteins is


pancreaticenzymes: peptidase, lipases, nucleases & esterases.
 These are secreted in considerable quantity into the intestinal
lumen and rapidly hydrolyses macromolecules and lipids.
 Enzymatic degradation brought about via 2 ways :-

1. Hydrolytic cleavage of peptide bonds by Insulin degrading


enzyme, ACE & Renin.
 Proteolysis is irreversible reaction and hence causes
damage of peptides and protein drugs.

2. Chemical modification of protein such as phosphorylation by


kinases, oxidation by xanthine oxidase or glucose oxidase.
 It limits absorption of protein drugs from GIT.
2. Intestinal Epithelial Barriers :-
 The intestinal epithelium is the single cell layer that form the
luminal surface (lining) of both the small and large intestine
(Colon) of the gastrointestinal tract composed of Simple
columnar epithelial cells supported by lamina propria
muscularis mucosa.

 Brush border is microvilli covered surface of cell found in


small intestine, these plays imp.role in nutrient digestion and
absorption.
 Tight junctions mediate the paracellular pathway of
absorption in intact membranes and are rate limiting step in
transepithelial transport.
3. Capillary Endothelial Barriers :-

 To cross capillary endothelium the proteins must pass


between cells or alternatively transverse the endothelial cells
themselves.
 Solutes that transverse endothelial cell membrane may get
metabolised by cytoplasmic enzymes.
 Thus the endothelial passes enzymatic barrier to solution
package.
4. Blood brain barriers :-

 Represents major obstacal to brain compartments.

 Collection of cells that press together to block many


substances from entering the brain while allowing other to
pass.

 Allow passage to lipid mediated transport of small but


lipophilic molecules and gases.
 Large molecules like proteins donot pass the BBB early.
~: reference :~

 A TEXT BOOK OF DRUG DELIVAR SYSTEM


PUBALISHED BY PEEVEEPUBALICATION AUTHORIZE
BY PRAFULLN P. PATIL, BHUSHAN P. GAYAKWAD,
Dr.MD. RAGEEB MD.USMAN AND Dr. SUROJJ SARODE .
 Saba Saeed 1, Mavra Irfan 1, Saima Naz 2, Momil Liaquat 2,
Shafaq Jahan 2, Sana Hayat 2Routes and barriers associated
with protein and peptide drug delivery system 2021 Aug.
 www.google.com

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