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Lecture 8

Advantages of Pulmonary Drug Delivery

1. Used for local delivery of drugs to the lungs for asthma treatment.

2. Non-invasive route of systemic drug delivery.

3. Rapid absorption and fast onset of action (comparable to IV drug

4. Avoid harsh conditions of the GIT

5. Drug efflux transporters and metabolizing enzymes are present in
the lung at much lower levels than the gastrointestinal tract

Limitations to Pulmonary Drug Delivery

1. Inhaled drug particles must possess specific particle diameter in
order to pass from nose and mouth filters and at the same time
dispose inside the lung

2. Excipients used in drug formulation can cause irritation or
permanent injury to the lung.

3. High disposition of drug in the oro-pharynx region.

Why are peptides and proteins rapidly absorbed after inhalation
than after subcutaneous injection?

Rapid onset

High rate

High blood supply in alveolus barrier

Alveolus blood barrier is permeable

Very large absorptive surface area

No metabolic (degradative) enzymes

No efflux pumps

Very thin membrane (0.1-0.2 Micrometer)

Presence of protein binding sites

5µm: diffusion (Brownian motion)  Interaction forces: For drug particles to be flowable and easily dispensed. the size and the porosity by varying different . Factors affecting Pulmonary Drug Delivery Drug-related factors  Particle diameter: Drug particle size affects the mechanism of drug disposition into the lungs: • Drug particles in the range of 0.5-5µm: sedimentation • Drug particles> 5µm: gravity • Drug particles <0.  Drug dose  Drug concentration at target site. Microspheres can be produced following different requirements such as the morphology. Pulmonary Drug Delivery Devices Pulmonary drug carrier systems Biodegradable microspheres Pulmonary administration of aerosolized microspheres allows a sustained and prolonged release of drugs for respiratory or non respiratory diseases. interaction forces between drug particles must be overcome during drug particles preparation steps.

In this case. potentially reducing the . Size reduction can occur via a number of means. Lecture 9 Nanotechnology provides the following solutions to the problems of drug delivery: (Advantages)  Improving solubilization of the drug. Nanotechnology-based solutions to improve drug solubility: • When the particle size of a drug is reduced to the nanometre range.  Using non-invasive routes of administration eliminates the need for administration of drugs by injection. • The nanostructuring process creates a porous honeycombed structure that dramatically increases the carrier’s surface area. including milling or homogenization techniques. Microspheres are less hygroscopic and are then less liable to swell in the presence of moisture located into the lungs Nanotechnology in drug delivery New drug delivery areas in which nanotechnology efforts are being focused. the drug molecules are immobilized within the nanosized pores in the structure. which can be varied to carry a range of different sized molecules.  Development of nanoparticles formulations for improved absorption of insoluble compound and macromolecules enables improved bioavailability and release rates. thereby enhancing the solubility of the drug. the surface area is significantly increased. Why nanotechnology is used in poorly water soluble drugs? 1.technological parameters during their preparation.  Development of novel nanoparticle formulations with improved stabilities and shelf-lives. Improving solubility of poorly water soluble drugs.

and surface properties could be more efficient and less expensive than other technologies. The hydrocarbon tails of one layer face the hydrocarbon tails of the other layer.  Manufacture of nanoparticle formulations with controlled particle size.  Direct coupling of drugs to targeting ligands restricts the coupling capacity to a few drug molecules. and the combined structure forms a bilayer.  Nanoparticle formulations that can provide sustained release profiles up to 24 h can improve patient compliance with drug regimens. being of the same composition. Lipid bilayer of liposomes are similar in structure to those found in living cell membranes and can carry lipiphilic substances such as drugs within these layers. It is postulated that when they reach the outside of a living cell membrane they may become accepted as part of the membrane. amount of dose required and increasing safety through reduced side effects. attracted to the water in the environment. one layer of heads faces outside of the cell. Advantages of liposomes as drug delivery system . Liposome property vary with lipid composition. morphology. size. In a cell. Another layer of heads faces inside the cell. attracted by the water inside the cell. but coupling of drug carrier nanosystems to ligands allows input of thousands of drug molecules by means of one receptor targeted ligand. They act as a carrier for the enclosed substances. in the order of a nanometer. The size of these spheres is very small. Liposomes Liposomes are stable vesicles formed by phospholipids and similar amphiphilic lipids. Liposomes can be conjugated to antibodies or ligands to enhance targeting of specific drug or gene therapy. surface charge and the method of preparation.

or both. These liposomes are used for gene therapy. This is accomplished by highly specific chemical modifications to the PEG molecules or the lipid bilayer of the liposomes. Liposomes have the ability to protect their encapsulated drug from the external environment and to act as sustained release depots (Propranolol. Suitable for delivery of hydrophobic and hydrophilic drugs and agents. Cyclosporin). Flexibility to couple with site-specific ligands to achieve active targeting (Anticancer and Antimicrobial drugs). Cationic liposomes: are stealth liposomes whose surfaces (both exterior and interior) are positively charged so as to increase the loading efficiency of recombinant DNA. completely biodegradable. Liposomes are biocompatible. flexible and non-immunogenic for systemic and non- systemic administrations. non- toxic. Four kinds of liposomes Immunoliposomes: are stealth liposomes that have been specially designed for active targeting to a given type of tissue or organ that the liposome is able to recognize by its molecular fingerprint. in which certain disorders are treated by introducing specifically engineered genetic material (DNA) into the patient’s cells through active targeting. .