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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PRESENTED BY
MONIKA TARGHOTRA
M.PHARM (2 SEM )
PHARMACEUTICS
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2.  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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3.  Erythropoietin used for production of RBC.
 Tissue plasminogen activator is used for Heart attack, Stroke.
 Oxytocin maintain 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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4. The structure of protein divided in to four types:
1. Primary structure : It denotes the number and sequence of amino acids in
the protein. It is maintained by the covalent bonds of the peptide linkage.
2. Secondary structure: It refers to the local three dimensional folding of the
polypeptide chain in protein . These are mainly stabilized by the weak non
covalent interactions.
3. Tertiary structure : It refers to the three dimensional structure of
polypeptide.
4. Quaternary structure : Protein that contains two or more polypeptide
chains associated by non covalent forces are said to be exhibit quaternary
structure.
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6.  Parenteral route is most efficient way for systemic delivery of
proteins and peptides.
 This is the best choice to achieve therapeutic activity.
 ADVANTAGES-
1.allow rapid and complete absorption.
2.Avoid first pass metabolism.
 DISAVANTAGES-
1. problems with overdosing , necrosis
2. Hypersenitivity reactions.
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7.  Polymer based drug delivery system.
 Liposome based drug delivery system.
 Hydro gel based drug delivery system.
 Emulsion based drug delivery system.
PUMPS:
 Implantable infusion pumps
 Mechanical pumps
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8. CHARACTERS OF POLYMERS
 It should be biodegradable.
 It should be bio compatible.
 It should be non-toxic.
Two types of polymers are used widely
 natural polymers- collagen, gelatin, casein.
 synthetic polymers- polyglcolic acid, polylactic acid.
 NANOPARTICLES with moeities like monoclonal antibodies, are
being used for the targeted delivery of peptides and proteins .
Polymers used for preparation of nanoparticles include albumin,
acrylic resins, chitosan, polystyrene etc.
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9.  Spherical vesicles with a phospholipid bilayer
 Liposome's are microscopic vesicles composed of one or more aqueous
compartments.
Liposome’s in Proteins delivery :
 Example: Lecithin used in controlled drug release.
Liposome’s in peptide drug delivery:
 Bleomycin : A peptide with anti tumor activity, reduces normal tissue
toxicity.
 Negatively charged liposome's produces a prolonged hypoglycemic effect
in diabetic drugs, which are injected by subcutaneous injection.
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10. ADVANTAGES OF LIPOSOME DRUG DELIVERY
 Soluble in both organic and aqueous media.
 Liposome’s are important for targeting drugs directly to the liver, and
brain.
 Liposomes easily crosses blood brain barrier.
EXAMPLE: Dopamine converted to L-Dopa.
 Used as a vehicles for vaccines.
DISADVANTAGES
 Less stable , easily susceptible to oxidation.
 Hence liposome’s are replaced by noisome an alternate for liposome’s.
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11. Hydrogels are three dimensional networks of hydrophilic polymers
that are insoluble.
 Hydro gels are polymers which have the ability to swell in water .
 Biodegradable hydro gels are used, due to its biocompatibility .
 Hydrogels are highly biocompatible, and a feasible approach ti
incorporate drugs into matrices.
Examples:
Hydroxymethylacrylate, used to minimize mechanical irritation to
surrounding tissue.
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12. EMULSION BASED DELIVERY
 Emulsions can be used for parenteral drug delivery of proteins and
peptides used to prolong the release of drug.
 example-subcutaneous administration of muramyl dipeptide in a w/o
emulsion. It is used to potentiate immune system.
CELLULAR CARRIERS
 Protein and peptides can be incorporated in erythrocytes to achieve the
prolong release or targeting.
 Resealed erythrocytes as delivery system for C- reactive protein to
generate macrophages , and mainly used to target liver and spleen.
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13. PUMPS
Types of pumps:
1. IMPLANTABLE PUMPS
 Drug is implanted subcutaneously, and delivered by I.V infusion.
 Pumps are filled with drug through a septum with a needle.
 Pumps deliver drugs to central vein for 7-14 days a constant rate.
2. MECHANICAL PUMPS
 Easily manipulated to deliver protein and peptide drugs.
Example: insulin has been successfully delivered by portable syringe.
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14. NON PARENTERAL ROUTES OF ADMINISTRATION
Parenteral route is not properly achievable, hence other routes are preferred
 Oral route.
 Rectal route.
 Nasal route.
 Pulmonary route.
 Buccal route.
 Transdermal route.
 Ocular route
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15. ORAL ROUTE
 Encapsulated peptides or proteins in amino acids with
microsphere of approximately 10 micron in diameter , used for
oral delivery.
Example: Insulin and heparin.
 Orally administered insulin produces hypoglycemic effect .
DISADVANTAGES:
 Acid catalyzed degradation in stomach.
 Proteolysis in GIT.
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16.  This is topical drug delivery system.
 Drug is absorbed through the skin.
 EX: Insulin, vasopressin
ADVANTAGES:
 Controlled administration of drug is possible.
 Improved patient compliance.
 Drugs with short half lives can be administered.
DISADVANTAGES:
 High intra and inter patient variability.
 Low permeation because of high molecular weight.
 Hydrophilicity and lipophilicity of stratum corneum.
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17. Number of approaches are available for effective protein and peptide drug delivery.
They are as follows-
 Iontophoresis
 Phonophoresis
 Penetration enhancer
These are described as follows-
 Iontophoresis -Used for local and systemic delivery of proteins and peptides. In
this an electric current is used to drive the molecules across the skin surface.
Example: Transport of insulin using iontophoresis.
 Phonophoresis- The absorption is enhanced by thermal effect of ultrasonic waves
and subsequent alteration of physical structure of skin surface.
 penetration enhancer-these are applicable to improve the membrane permeations
of large macromolecular substsances . Permeation enhancer used are dimethlyl
sulfoxide , oleic acid, surfactants, azones and terpenes etc.
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18.  Lungs are attractive site for systemic delivery of proteins and peptides
because of their enormous surface area(70 sq.m)
 Alveoli and lungs are the absorption sites.
 Drugs are absorbed through lungs by simple diffusion, carrier mediated
transport
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19. ADVANTAGES:
 Decrease in dose requirement.
 Fast absorption
 Increased patient compliance
DISADVANTAGES:
 Inflammation may be observed in lungs.
 Degree of bioavailability was less due to hydrolytic enzymes present in
lungs.
 EXAMPLE- albumin was largely absorbed within 48 hours of
installation into the lungs of guinea pigs.
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20.  Rectum is highly vascularised body cavity.
 Rectal mucosa is devoid of villi.
 Drugs are in form of suppositories, gel, dry powders.
EX: Insulin, calcitonin
ADVANTAGES:
 Reduced proteolytic degradation.
 Improved systemic bioavailability with co-administration of absorption
enhancers.
Example : surfactants
 Large dose can be administered.
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21. OCULAR ROUTE
oTopically applied drugs reach the blood stream via the blood vessels in the
conjuctival sac
o In this route enkephalins, thyrotrophin releasing hormones ,luteinizing
hormones ,glucagon and insulin are administered
BUCCAL ROUTE
o Mucoadhesive dosage form can be used for buccal route.
o Adsorption enhancer like salicylate or surfactant is used for protein and
peptide delivery.
Example:
o Oxytocin , vasopressin , insulin, are reported to be absorbed through buccal
mucosa . And adhesive gel, patches , tablets are used.
o Insulin is absorbed through buccal mucosa in the presence of sodium
glycolate. 21

22.  The nasal route has been employed for producing local action on the
mucosa which is more permeable compared to oral mucosa.
 Nasal absorption is through passive diffusion.
EX: Insulin, human growth hormone.
ADVANTAGES:
 Rapid onset of action
 First pass metabolism can be avoided
 Better drug absorption
DISADVANTAGES:
 Long-term usage causes toxicity.
 Size of proteins and peptide drugs reduces systemic bioavailability.
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23.  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.
 Peptide and protein drugs will be produced on a large scale by
biotechnology processes and will become commercially available for
therapeutic use.
 Their need in the clinical & therapeutic regions has intensified the
investigation for their convenient & effective delivery through
noninvasive system.
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