Pandey, Shivanand and Bhatt, Sweta and Patel, Binal and Mahalaxmi, R and Devmurari, Viral and Jivani, NP (2009) Local and Systemic Pulmonary Drug Delivery of Small Molecules. Journal of Pharmacy Research, 2 (8). pp. 1200-1202.

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Abstract

Advancements in the development of ultra-fine drug molecules and peptides suitable for pulmonary delivery have created the requirement for novel handling, metering and drug dispensing techniques; while circumventing the problem of agglomeration (usually solved by mixing the active drug formula with Excipient. Inhalation has long been established in the treatment of respiratory diseases as an effective means of delivering drugs for local effect in the lungs. Local delivery of therapeutic agents offers the advantage of increased concentration at the site of action without the problems of systemic side effects. Recently, interest has increased in exploiting the lung’s ability to transfer molecules (i.e. proteins, peptides or other low solubility drugs) to the bloodstream for a systemic effect with a fast action, low first-pass metabolism(unlike GI route ) profile. Among the three main types of devices that are used to administer drugs to the lungs Dry Powder Inhalers (DPI’s) present the major advantage that they are breath activated, requiring no patient co-ordination during activation. (The lack of a patient’s co-ordination of breathing with activating an inhaler is recognized as one of the main causes for lack of compliance and of inconsistent or sub-optimal dosing, a serious problem with drug treatments that feature a narrow therapeutic window). To deliver pharmaceuticals to (local) or through (systemic) the lungs, drugs must be transformed into an aerosol that can be inhaled by the patient. If an aerosol is to be delivered to the deep lung, the individual particles must be small and their velocity must be low as they pass through the upper airways and into the deep lung. With a DPI, the particle velocity is controlled by the patient’s breath unlike for metered dose inhalers that emit medication under pressure and at high speed.

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