PULMONARY

DRUG DELIVERY
ROUTE
 Introduction
• It provides a large surface area for drug absorption
• This route has unique advantages over other
routes.
• It has gained importance as a drug delivery system
Anatomy of Respiratory system
 Advantages of Pulmonary Route
• Has a fast onset of action
• Avoids first pass metabolism
• Non invasive (needle free)
• Dose to produce effect can be reduced
• Large surface area for drug absorption
 Barriers of Pulmonary Drug
Delivery
Mechanical barriers
a. Removal of drug by mucociliary system
b. Impaction of drug in mouth.

Chemical barriers
c. Breakdown by enzymes
d. Effect of surfactants
Immunological barriers
a. Engulfment by alveolar macrophages

Personal/Behavioral barriers
b. Non adherence to treatment
c. Poor inhalation techniques
 Factors affecting drug absorption
and bioavailability
Physicochemical properties
 Solubility
Increased solubility increases dissolution.
Increase in dissolution increases absorption.

Particle size
It is inversely proportional to absorption.
Salt form
The salt form of a drug has a greater dissolution.
This leads to increased absorption.

 Solvates and hydrates

Solvates have a higher dissolution in fluids.
Ph
It affects the degree of ionization of the drug.

Lipophilicity.
Highly lipophilic drugs have high bioavailability .
They cross the cell membrane easily.
 Formulation factors
Includes
a. Disintegration time
b. Manufacturing variables
c. Product age and storage conditions
d. Excipients used
Devised used to deliver medication are
a. Metered Dose Inhalers(MDIs)
b. Dry powder inhalers(DPI)
c. Nebulizers
 Biopharmaceutical Analysis
• Invitro studies
Dissolution test
Tests rate at which the drug enters into solution.
Can predict the bioavailability of the drug.
Disintegration test
Predict the rate at which particles disintegrate.
Can predict bioavailability.
 • Invivo studies
Plasma level studies
Plasma concentration equals amount administerd

Urinary excretion studies

Applicable to drugs excreted unchanged-renally.
Can predict plasma concentration.
 An example of drug formulation
delivered via pulmonary route
 Salbutamol formulated as an inhaler
 Used in management of asthma.
Delivery involves use of MDI
Spacers increase efficiency of delivery.
The excipients to use include

Propellants -eg chloroflourocarbons(CFCs).

Used to propel the drug.
Can react with the API and the container.
CFCs are also not environment friendly.
• Surfactant- used to provide lubrication.
interacts with API enhancing lipophilicity.

• Cosolvent- used as formulation aid.

React with API and excipients.
• Preservatives- prevent microbial spoilage.
Can chemically react with the API

• Humectants- absorb moisture

prevent hydrolysis of API by moisture.
 Conclusion
• Has large surface area for absorption.
• It is also highly vascularized.
• Offers rapid onset of drug action.
• it is ideal for use in drug administration.
• Route should be explored further.
 References
Amidon, Seth; Brown, Jack E.; Dave, Vivek S. (August
2015). "Colon-Targeted Oral Drug Delivery Systems:
Design Trends and Approaches". AAPS PharmSciTech.
16 (4): 731–741.

Jain, Kewal K. (2020), Jain, Kewal K. (ed.), "An

Overview of Drug Delivery Systems", Drug Delivery
Systems, Methods in Molecular Biology, New York,
NY: Springer New York, vol. 2059, pp. 1–54

Li, Chong; Wang, Jiancheng; Wang, Yiguang; Gao,

Huile; Wei, Gang; Huang, Yongzhuo; Yu, Haijun; Gan,
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