The document discusses protein and peptide drug delivery systems. It describes proteins and peptides, their uses in pharmaceuticals like insulin, and challenges in delivering them orally due to enzymatic and epithelial barriers. Various formulation vehicles that can help deliver proteins and peptides orally are described, including dry emulsions, microspheres, liposomes and nanoparticles. The document also covers evaluating protein and peptide drug formulations through methods like stability testing, bioassay, and chromatography.
pH-activated and Enzyme-activated drug delivery systemSakshiSharma250807
As per the syllabus of M.Pharma (1st sem.) I have presented the topic pH-activated and Enzyme-activated. This comes under rate-controlled drug delivery system under the subject Drug delivery system. Best wishes from Sakshi Sharma
Gastro retentive drug delivery systems by shubham patilShubham Patil
General Discussion on Drug delivery System specially focused on Gastro-Retentive. I've covered various types and theories & understandably prepared this presentation for everyone who reads it.
pH-activated and Enzyme-activated drug delivery systemSakshiSharma250807
As per the syllabus of M.Pharma (1st sem.) I have presented the topic pH-activated and Enzyme-activated. This comes under rate-controlled drug delivery system under the subject Drug delivery system. Best wishes from Sakshi Sharma
Gastro retentive drug delivery systems by shubham patilShubham Patil
General Discussion on Drug delivery System specially focused on Gastro-Retentive. I've covered various types and theories & understandably prepared this presentation for everyone who reads it.
Barriers to Protein and peptide drug delivery system JaskiranKaur72
Protein and peptide DDS are novel systems of drug 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 milieu. Various barriers encountered are-
1 Physiological Barrier
2 Intestinal Epithelial barriers
3 Capillary Endothelial Barrier
4 Blood-Brain barrier (BBB)
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Aquasomes are nanoparticulate carrier system but instead of being simple nanoparticles these are three layered self assembled structures, comprised of a solid phase nanocrystalline core coated with oligomeric film to which biochemically active molecules are adsorbed with or without modification.
PROTEINS: Proteins are the organic compounds made of amino acids and joined together by peptide bonds.
PEPTIDES: These are short polymers formed from the linking in a defined order of amino acids.
Protein and peptides are the most abundant material which act as hormones, transport protein, structural protein, receptor, immunoglobulin’s in living system and biological cell.
Protein and peptides are important part in several metabolic process, immunogenic defense and many other biological activities.
Protein and peptide use in the treatment of various diseases including Endocrine dysfunction, Infection diseases, Cancer, and CNS disorders.
According to their biological roles
Enzymes- Catalyses virtually all chemical reaction
Transport proteins i.e. Haemoglobin of erythrocytes
Defense proteins i.e. Immuno globulins Antibodies
Structural proteins i.e. Collagen in bones
Regulatory proteins i.e. insulin
Nutrient and storage proteins i.e. ovalbumin
According to their solubility
Globular proteins: Soluble in Water
Fibrous proteins: Insoluble in water
WHY PROTEN AND PEPTIDE DRUGS?
The protein and peptide are very important in biological cells.
Lack of proteins and peptides causes diseases like Diabetes mellitus.
Diabetes mellitus is cause due to the lack of protein called INSULIN.
Now a day R-DNA technology and hybridoma also use in protein and peptide based pharmaceuticals.
FUNCTIONS
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.
Problems with proteins
Elimination by B and T cells.
Proteolysis by endo/exo peptidases.
Small proteins filtered out by the kidneys very quickly.
Unwanted allergic reactions may develop (even toxicity).
Loss due to insolubility/adsorption.
Barriers to Protein and peptide drug delivery system JaskiranKaur72
Protein and peptide DDS are novel systems of drug 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 milieu. Various barriers encountered are-
1 Physiological Barrier
2 Intestinal Epithelial barriers
3 Capillary Endothelial Barrier
4 Blood-Brain barrier (BBB)
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Aquasomes are nanoparticulate carrier system but instead of being simple nanoparticles these are three layered self assembled structures, comprised of a solid phase nanocrystalline core coated with oligomeric film to which biochemically active molecules are adsorbed with or without modification.
PROTEINS: Proteins are the organic compounds made of amino acids and joined together by peptide bonds.
PEPTIDES: These are short polymers formed from the linking in a defined order of amino acids.
Protein and peptides are the most abundant material which act as hormones, transport protein, structural protein, receptor, immunoglobulin’s in living system and biological cell.
Protein and peptides are important part in several metabolic process, immunogenic defense and many other biological activities.
Protein and peptide use in the treatment of various diseases including Endocrine dysfunction, Infection diseases, Cancer, and CNS disorders.
According to their biological roles
Enzymes- Catalyses virtually all chemical reaction
Transport proteins i.e. Haemoglobin of erythrocytes
Defense proteins i.e. Immuno globulins Antibodies
Structural proteins i.e. Collagen in bones
Regulatory proteins i.e. insulin
Nutrient and storage proteins i.e. ovalbumin
According to their solubility
Globular proteins: Soluble in Water
Fibrous proteins: Insoluble in water
WHY PROTEN AND PEPTIDE DRUGS?
The protein and peptide are very important in biological cells.
Lack of proteins and peptides causes diseases like Diabetes mellitus.
Diabetes mellitus is cause due to the lack of protein called INSULIN.
Now a day R-DNA technology and hybridoma also use in protein and peptide based pharmaceuticals.
FUNCTIONS
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.
Problems with proteins
Elimination by B and T cells.
Proteolysis by endo/exo peptidases.
Small proteins filtered out by the kidneys very quickly.
Unwanted allergic reactions may develop (even toxicity).
Loss due to insolubility/adsorption.
Protein and peptide are biopolymers which yield more than two amino acids on hydrolysis.
Although the terms ‘proteins’ and ‘peptides’ are used freely, peptides are those with molecular weight below 10,000 and proteins are molecules with higher molecular weight.
Most therapeutic proteins and peptide-based drugs are administered by parenteral route and are incorporated in liposomes to prolong their action or fused with Immunoglobulins or Albumin to improve their half-life.
PEGylation is a proven technique for improving the potentials of Proteins/peptide delivery systems.
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.
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
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Pharmacokinetics and pharmacodynamics of biotechnological drugs along with appliations- Proteins and peptides, monoclonal antibodies, oligonucleotides, gene therapy and vaccines
DOWNLOAD THE POWERPOINT FILE HERE:
https://www.dropbox.com/s/3izi11rbc7axri3/CHE-109.pptx?dl=0
A presentation slide on Peptides and Proteins. Presented in the Course CHE-109 in East West University.
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
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1. Protein and peptide drug
delivery system
UNDER THE GUIDENCE OF, PRESENTED BY
DR.ANUPRIYA KAPOOR SHIVANI SINGH
ASSISTANT PROFESSOR M.PHARMA 1ST YEAR
SCHOOL OF PHARMACEUTICAL SCIENCE
CSJMU , KANPUR
2. INTRODUCTION
Protein: Proteins are the large organic compound made of amino acids
arranged in a linear chain 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. Why protein and peptide are used
The protein and peptide are very important in biological
cells.
Lack of proteins and peptides causes disease like diabetes
mellitus.
Diabetes mellitus is caused due to the lack of protein called
INSULIN.
Now a days R- DNA technology and hybridoma techniques
also used in protein and peptide based pharmaceuticals.
4. ADVANTAGE
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.
5. DISADVANTAGE
Very large and unstable molecules.
Structure is held together by weak non- covalent
forces.
Easily destroyed by relatively mild storage conditions
and gastric juices.
Hard to obtain in large quantities.
6. FUNCTIONS
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.
7. 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 protein.
8.
9. Classification of protein and peptide
Depending on the number of amino acids they are
classified as follows:
1. Polypeptides protein
2. Oligopeptides protein
3. Fibrous protein
4. Globular protein
5. Oligo meric protein
10.
11. Barriers to protein and peptide
delivery
The successful delivery of protein and peptide based
pharmaceuticals is primarily determined by its ability to
cross the various Barriers presented to it in the biological
milieu. Various Barriers encountered are –
Enzymatic Barriers
Intestinal Epithelial Barriers
Capillary Endothelial Barrier
Blood Brain Barrier (BBB)
12. Enzymatic Barriers
Major Enzymatic Barrier to absorption of proteins is
pancreatic enzymes : peptidase, lipases, nucleases and
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
2. Chemical modification
13. Intestinal Epithelial Barriers
The majority of peptide degradation occurs in the brush
border membrane.
Brush border is microvilli covered surface of cell found in small
intestine, these plays important role in nutrient digestion and
absorption .
Tight junctions mediate the paracellular pathway of
absorption in intact membrane and are rate limiting step in
transepithelial transport.
15. Capillary Endothelial Barrier
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.
16. Blood Brain Barrier (BBB)
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.
18. Formulation vehicles
The protein and peptide drug delivery system is important
for the oral delivery of protein and peptide can be
successfully achieved by using various carrier systems
are like –
1. Dry Emulsion
2. Microspheres
3. Liposomes
4. Nanoparticles
19. Dry Emulsion
It is important application in drug delivery system to
prevent the instabilities of the long term storage of
multiple emulsions.
The novel approach at which multiple emulsion is
replaced by dry emulsions.
In dry emulsion preparation application of the PH
responsive polymers like HPMC, is important for the
emulsion are the enteric coated and sites specific
achieved.
20. Microspheres
The uniform distribution of drug in oral drug delivery in
protein peptides drug are known as microspheres.
The PH responsive microspheres are the mainly used in
oral delivery for the protection of the stomach from
proteolytic degradation and protection upper portion
of small intestine from proteolytic degradations
21. Liposomes
Liposomes are the small microscopic vesicles in which
aqueous volume is entirely enclosed by the membrane
composed lipid molecules.
Liposomes in drug delivery system, the encapsulation of
the insulin with sugar chain portion of mucin and PEG
completely suppressed the degradation of the insulin
molecules in intestinal fluid.
22. Nanoparticles
Nanoparticles are nano sized colloidal structure having
size is 10-1000nm.
The particles in nanometric sized range of the particles
are absorbed intact by the intestinal epithelium and
they are the less prone towards the enzymatic
degradation.
The particle size surface charges are the influencing the
uptake of nanoparticle system in GI tract.
23. Evaluation of protein and peptide drug
formulation
Stability testing
Bioassay
UV spectroscopy
Bradford assay
Differential scanning calorimetry
Chromatography
Electrophoresis
24. Reference
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
