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Pulmonary drug delivery system
The document discusses pulmonary drug delivery, emphasizing its application for treating respiratory conditions like asthma and COPD through inhalation therapies and sophisticated delivery devices. It outlines the advantages, such as reduced side effects and targeted drug action, alongside various challenges, including device efficiency and physiological barriers. Recent technological advances like nebulizers and dry powder inhalers enhance treatment effectiveness by improving drug formulation and delivery mechanisms.
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Pulmonary drug delivery system
- 1. 1 Presented by- Mr. SachinM.Chandankar M. Pharm Department of Pharmaceutics
- 2. • Introduction • Anatomyof lungs • Advantages • Disadvantages • Challenges • Factors affecting • Barriers • Formulation approches • Containers • Evaluations • Applications • Marketed Products • Newer Developments • Conclusion • References 2
- 3. • Pulmonary drugdelivery is primarily used to treat conditions of the airways,delivering locally acting drugs directly to their site of action. • The inhalation therapies involved the use of leaves from plants, vapours from aromatic plants, balsams, and myhrr. • The drug used for asthma and COPD e.g..- β2-agonists such as salbutamol (albuterol), Terbutalin formoterol, corticosteroids such as budesonide, beclomethasone and mast-cell stabilizers such as sodium cromoglycate or nedocromi. 3
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- 5. • The doseneeded to produce a pharmacological effect can be reduced. • Low concentrations in the systemic circulation are associated with reduced systemic side-effects. • Rapid onset of action. • Avoidance of gastrointestinal upset. • Avoidance of intestinal and hepatic first-pass metabolism. • Deliver high drug concentrations directly to the disease site. 5
- 6. • Complex deliverydevices are required to target drugs to the airways and these devices may be inefficient. • Aerosol devices can be difficult to use. • Various factors affect the reproducibility of drug delivery to the lungs, including physiological (respiratory maneuver) and pharmaceutical (device, formulation) variables. • Drug absorption may be limited by the physical barrier of the mucus layer and the interactions of drugs with mucus. • Mucociliary clearance reduces the retention time of drugs within the lungs. 6
- 7. • Low efficiencyof inhalation system particle size-0.5-1mm • Less drug mass per puff less than 1000 mcg • Poor formulation stability for drug • Improper dosing reproducibility 7
- 8. Physiological factors 1. Thicknessof Mucous layer 2. Lung morphology 3. Pulmonary surfactant 4. PH of microenvironment 5. Surface area 6. Tidal volume 7. Blood flow 8 Physico-chemical factors 1. Lipid solubility 2. Pka 3.Particle size (1-3 um) 4. Density -0.4 g cm3 5.Electric charge 6.Shape 7. Hygroscopy Formulation factor 1. Use of excipient 2. Type of formulation 3.Combination thereapies 4.Aerosol velocity
- 9. Mechanical barriers • Coughing •Sneezing • Mucous • Ciliary cells • Pulmonary epithelium ( Thick layer 5-10um) Chemical barrier • Surfactant • Pulmonary metabolism Immunological barriers • Alveolar macrophages 9
- 10. • Pulmonary delivereddrugs are rapidly absorbed except large macromolecules drugs, which may yield low bioavailability due to enzymatic degradation and/or low mucosal permeability. • Pulmonary bioavailability of drugs could be improved by including various permeation enhancers such as surfactants, fatty acids, saccharides, chelating agents and enzyme inhibitors such as protease inhibitors. Recent advances in Formulations- • Micronization via jet milling, • Precipitation, • Spray drying using various excipients, such as lipids and polymers,Carrier systems like lactose. • Liposomes, • Nanoparticles. 10
- 11. 11 •Definition- A suspensionof very fine liquid or solid particles in a gas. •Respirable range:1-5 micron •80%drugs deposited in oropharynx •10% in walls of inhaler •10% in the lungs • The drugs, delivery • by aerosols is deposited in the airways by: 1.Inertial impaction-greter than 1um 2.Gravitational sedimentation- 0.5um 3.Diffusion-lesst han 1um
- 12. Recent technologies ofpulmonary drug delivery- 1. NEBULISERS a) Jet Nebulisers b)ultrasonic nebulizers 2. DRY-POWDER INHALER (DPI) a)Unit dose Devices b)Multidose Devices 3.METERED–DOSE INHALER (MDI) 12
- 13. • A nebulizeris a device used to administer medication to patient in the form of a mist inhaled into the lungs. • Used in treating cystic fibrosis, asthma, and other respiratory diseases. • There are two basic types of nebulizers: • The jet nebulizer functions by the Bernoulli principle by which compressed gas (air or oxygen) passes through a narrow orifice, creating an area of low pressure at the outlet of the adjacent liquid feed tube. This results in the drug solution being drawn up from the fluid reservoir and shattering into droplets in the gas stream. • The ultrasonic nebulizer uses a piezoelectric crystal, vibrating at a high frequency (usually 1–3 MHz), to generate a fountain of liquid in the nebulizer chamber; the higher the frequency, the smaller the droplets produced. 13
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- 15. • DPIs arebolus drug delivery devices that contain solid drug in a dry powder mix that is fluidized when the patient inhales. • They typically formulated as one-phase, solid particle blends. The drug with particle sizes of less than 5µm is used. • Either they contain the active drug alone or have a carrier powder (e.g. lactose) mixed with the drug to increase flow properties of drug. • They are a widely accepted particularly in Europe, where they are currently used by approximately 40% of asthma patients. There are two types of devices- 1. Unit dose Devices Single dose powder inhalers are devices in which a powder containing capsule is placed in a holder. The capsule is opened within the device and the powder is inhaled. 2.Multidose Devices This device is truly a metered-dose powder delivery system. The drug is contained within a storage reservoir and can be dispensed into the dosing chamber by a simple back and forth twisting action on the base of the unit. 15
- 16. Principal of drypowder inhaler design 16
- 17. •The pMDI containersmust withstand high pressure generated by the propellant. Stainless steel has been used as pMDI container material. Aluminium is now preferred because, compared to glass, it is lihgter, more compact, less fragile, and light proof. • In pMDI’s, drug is either dissolved or suspended in liquid propellants together with other excipients and presented in pressurized cantainer fitted with metering valve. • The predetermined dose is released as a spray on actuation of the metering valve. 17
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- 19. Containers:- Aerosol containermust withstand pressure as high as 140-180 psig at 130°F. Aerosols conatiners- A.Metals 1.Tinplated steel 2.Aluminium 3.Stainless steel B.Glass. 1.Uncoated glass 2.Plastic Coated 19
- 20. C. Valves AssemblyConsists of; 1.Ferrule or mounting cup 2.Valvebody or housing 3.Stem 4.Dip tube 5.Rubber ring D. Actuatores- 1.Sprey actuators 2.Foam actuators 3.Solid steam actuators 4.Special actuators 20
- 21. Containers Looking Ultra sonicnebulizer Jet nebuliser Dry powder inhaler 21
- 22. Properties Methods 1.Biological testing1.Therapeutic Activity 2.Toxicities Study B. Biological Characteristics 22 Properties Methods 1.Vapor Pressure 1.Pressure gauge 2.Density 1.Hydrometer 2.Pycnometer 3.Identification of Propellents 1.IR Spectroscopy 2.Gas Chromatography 4.Visual Evaluation 1.Rotational Viscometer 5.Particle Size Determination 1.Cascade Impactor 2.Light Scattering Decay A.Physiochemical Characteristics and Performance
- 23. 23 Particle Size Determination- 1.Cascade Impactor 2. Light Scattering Decay. a). Cascade Impactor- Principle- Stream of particles projected through a series of nozzles and glass slides at high velocity, larger particle are impacted first on lower velocity stage and smaller particles are collected at higher velocity stage. b). Light Scattering Decay- Principle- As aerosol settles under turbulent conditions, the change in the light intensity of a Tyndall beam is measured.
- 24. • In Asthmaand COPD-eg. bronchodilators corticosteroids. •Recent role pulmonary delivery in patients on ventilators. • In cystic fibrosis I- eg. N-Acetylcysteine. •In migraine- eg. Ergotamine. • In the Gene therapy via pulmonary route-eg. Cationic-lipid-mediated CFTR gene transfer can significantly influence the underlying chloride defect in the lungs of patients with CFC. •In angina pectoris –eg. Nitroglycerine. •In diabetes mellitus-eg. Insulin nanoparticals. 24
- 25. Dr Reddy's launches'Dose Counter Inhalers' in India Friday, April 16, 2010 Dr.Reddy's Laboratories (DRL) has launched an innovation in the metered dose inhaler (MDI) space with launch of 'Dose Counter Inhalers (DCI) for the first time in India. This the first MDI in India that gives patients an advance indication of when the inhaler is going to be empty. DCI is a new drug delivery device with a single device having 120 metered doses. There is a window in the inhaler that changes colour from green to red. Green indicates the inhaler is full, and red indicates the inhaler is empty. 25
- 26. Active ingredient BrandName Manufacturer Country Terbutaline 0.25mg Bricanyl AstraZeneca UK Beclomethasone dipropionate 250mcg Becloferte Cipla India Salbutamol Salbutamol Dry Powder capsules Cipla India Active ingredient Brand Name Manufacturer Country Salbutamol pressurized inhalation (100mcg) Asthalin Cipla India Albuterol Ventolin Gsk India Levalbutarol Xopenex 3D Pharmaceuticals U.S.A. Metered Dose inhaler Dry Powder Inhaler 26
- 27. • Pulmonary drugdelivery is an important research area which impacts the treatment of illnesses including asthma, chronic obstructive pulmonary disease and various diseases. • Regional drug targeting is now possible. • Local application is advantageous by pulmonary route. • Inhalation gives the most direct access to drug target. 27
- 28. • John J.Sciarra, Christopher J. Sciarra, Aerosols. In: Alfonso R. Geearo, editor. Remington: Science and practice of pharmacy, second edition.vol-1.New York: Lippincott Williams and Wilkins publication; 2001.p.963-979. • Anthony J. Hickey, Physiology of airway. In: Anthony J. Hickey, editor. Pharmaceutical inhalation aerosols technology, second edition.vol-54.New York: Marcel Dekker;1992.p.1-24. • Jain N. K, “Advances in Controlled and Novel Drug Delivery” 1st ed.(2010), CBS Publishers and Distributors Pvt.Ltd. New Delhi, p.120-156. • Lachman L, Liberman HA, Kaing JL, and Cuttie AJ. The theory and practice of Industrial Pharmacy, 3rd edition, Varghese Publishing House;1976. p.589 618. • Indian Pharmacopiea, 2014, Vol-1; p.24. • Pharmaceutical dosage form; Disperse system. Vol-3, p.495-498. 28
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