Controlled Release Drug Delivery Systems - An Introduction
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This document discusses controlled release drug delivery systems (CRDDS). It begins by defining CRDDS and comparing them to conventional drug delivery systems. CRDDS aim to control the rate, localization, and targeting of drug action in the body. The document then covers the history and classifications of CRDDS, including classifications based on technical sophistication, administration route, and other criteria. Various design considerations for CRDDS are outlined as well. Recent innovations in oral, nasal, ocular and transdermal delivery are also mentioned.
Controlled Release Drug Delivery Systems - An Introduction
- 1. CONTROLLED RELEASE DRUG DELIVERY SYSTEMS Al Ameen College of Pharmacy BY: SURAJ CHOUDHARY M.PHARM (PHARMACEUTICS) DEPT. OF PHARMACEUTICS
- 2. 2 PPT. PACKAGE CONTENTS:- THEME QUESTION -1 THEME QUESTION -2 FLASHBACK COMPARISON - 1 COMPARISON - 2 MOVEMENT RESTRICTIONS CRDDS DESIGN CONSIDERATIONS PRE-REQUISITES CLASSIFICATION CONCEPT-BASED ON CLASSES RECENT INNOVATIONS
- 3. 3 THEME QUESTION - 1
- 4. 4 What is DRUG DELIVERY SYSTEM?
- 5. 5 THEME QUESTION - 2
- 6. • Definition covers : ….. Controlled rate Localize drug action Target drug action 6 What is CONTROLLED RELEASE DDS?
- 7. FLASHBACK 7
- 8. 8 HISTORY ¤ The history of controlled release technology is divided into three time periods: 1950 to 1970 - Period of SUSTAINED DRUG RELEASE 1970 to 1990 - NEEDS of the control drug delivery 1990 (post era) - MODERN ERA of controlled release technology
- 9. COMPARISON - 1 CONTROLLED RELEASE DRUG DELIVERY SYSTEMS (CRDDS) Vs. CONVENTIONAL DRUG DELIVERY SYSTEMS (CONVENTIONAL) 9
- 10. 10 CRDDS VS CONVENTIONAL
- 11. CRDDS VS CONVENTIONAL • Conventional Periodic administration Non-specific administration High systemic concentrations can be toxic, causing side effects or damage to organs. Low concentrations can be ineffective. • CRDDS 11 Drug Concentration rises quickly to effective level. Effective concentration is maintained for extended time.
- 12. • Conventional Inconvenient Difficult to monitor Careful calculation necessary to prevent overdosing Large amounts of drug can be “lost” when they don’t get to the target organ Drug goes to non-target cells and can cause damage Expensive (using more drug than necessary) 12 DISADVANTAGES OF CONVENTIONAL
- 13. COMPARISON - 2 CONTROLLED RELEASE DRUG DELIVERY SYSTEMS (CRDDS) Vs. SUSTAINED RELEASE DRUG DELIVERY SYSTEMS (SR) 13
- 14. 14 CRDDS VS SR
- 15. • Sustained Release Controlled drug delivery Well - characterized and reproducible dosage form Controls entry to the body according to the specifications of the required drug delivery profile. (rate and duration of delivery are designed to achieve desired concentration) CRDDS VS SR • CRDDS 15 Release of drug is extended in time Rate and duration are not designed to achieve a particular profile.
- 17. Cost of formulation Fate of CRDDS Biocompatibility Fate of polymer,etc. 17 CHALLENGES IN CRDDS Drug absorption, distribution and metabolism vary among individuals Individualized therapy Controlled release
- 18. CRDDS DESIGN CONSIDERATIONS 18
- 19. Route of delivery Target sites 1. Desired site for efficacy 2. Sites to avoid to minimize side effects Type of therapy 1. Acute or chronic – rate and duration e.g., 1 yr duration implant vs. antibiotic for acute infection Patient condition 1. Cognitive ability and memory 2. Physical condition – ambulatory, bedridden, etc. 19 DESIGN CONSIDERATIONS
- 20. Polymer design considerations 1. Physical properties Glass transition temperature Diffusion characteristics 2. Compatibility with active 3. Stability – must not decompose in storage 4. Biocompatibility of polymer and degradation products 5. Ease of formulation and fabrication 6. Mechanical properties are stable when drug is added 7. Cost Agent 1. Physicochemical properties 2. Stability 3. Solubility 4. Partitioning 5. Charge 6. Protein binding properties 20 DESIGN CONSIDERATIONS
- 22. 22 PRE-REQUISITES …… OF A RESPONSIVE DRUG DELIVERY SYSTEM
- 24. 24 MECHANISMS PARTITION DISSOLUTION DIFFUSION OSMOSIS EROSION SWELLING TARGETTIN G COMBINATION
- 26. Based on the…………… 26 CLASSIFICATION CRITERIA
- 27. 27 BASED ON THE TECHNICAL SOPHISTICATION Rate- Preprogrammed DDS Activation- Modulated DDS Feedback-Regulated DDS Site-Targeting DDS
- 28. Rate of release of the drug has been PRE-PROGRAMMED at specific rate profiles. Fick’s law of diffusion are often followed. 28 RATE-PREPROGRAMMED DRUG DELIVERY SYSTEMS Drug Reservoir Rate-Controlling surface Drug
- 29. 1. Polymer Membrane Permeation Ex: i. Norplant subdermal implant (levonorgestrol, encap/sd) ii. Occusert system (Pilocarpine – Ethylene acetate mem) iii. Transderm-Nitro (disp. Of Nitroglycerine-lactose triturate) 2. Polymer Matrix Diffusion Controlled Ex: i. Nitro-Dur (Nitroglycerin) ii. Compudose subdermal implant (Estradiol) 3. Polymer Micro-reservoir Partition Ex: i. Nitrodisc (Nitroglycerin) ii. Subdermal Synvro-Mate-C implant (Norgestomet-PEG 400) 29 RATE-PREPROGRAMMED DRUG DELIVERY SYSTEMS
- 30. Rate of release of the drug has been ACTIVATED by some physical, chemical or Bio-chemical processes. Or it may be activated even by the energy supplied externally. 30 ACTIVATION-MODULATED DRUG DELIVERY SYSTEMS Drug Reservoir Rate-Controlling surface Drug Energy Sensor
- 31. 1. Physical Means Osmotic pressure activated Ex: Acutrim Tab (PPA HCl) Hydrodynamic pressure activated Vapor pressure activated Ex: Infusaid pump (Heparin) Mechanically activated Ex: M.D.Nebulizer (Buserelin) Magnetically activated Ex: Hemisphere (Bovine serum albumin) Sonophoresis activated Iontophoresis activated Ex: Phoresor by Motion Control (for anti-inflammatory drugs) Hydration activated Ex: Valrelease Tab (Valium) 2. Chemical Means pH-activated Ion-activated Hydrolysis-activated 3. Biochemical Means Enzyme-activated Ex: Albumin microspheres (5- Fluorosil) Biochemical-activated 31 ACTIVATION-MODULATED DRUG DELIVERY SYSTEMS
- 32. 32 FEEDBACK-REGULATED DRUG DELIVERY SYSTEMS Rate of release of the drug has been activated by a triggering agent, such as biochemical substance (in the body) & also regulated by it’s concentration via some FEEDBACK mechanisms. Drug Reservoir Rate-Controlling surface Drug Biochemical responsive/Energy Sensor
- 33. 1. Bioerosion regulated Ex: Urea activated Hydrocortisone 2. Bioresponsive Ex: Glucose triggered Insulin 3. Self-regulating Ex: Glycosylated Insulin- Concanavalin A 33 FEEDBACK-REGULATED DRUG DELIVERY SYSTEMS
- 34. Proposed by Ringsdorf. Consists of following parts attached to the non-immunogenic & biodegradable polymer: 1. Site-specific targeting moiety 3. Drug moiety with spacer 2. Solubilizer 34 SITE TARGETTING DRUG DELIVERY SYSTEMS Drug Reservoir Rate-Controlling surface Drug Biochemical responsive/Energy Sensor Site-Targetting Moiety
- 35. 35 BASED ON THE ROUTE OF ADMINISTRATION
- 36. • Osmotic Pressure • Hydrodynamic Pressure • Membrane Permeation Microporous MP Gastric Fluid-Resistant Intestine-Targeted • Gel Diffusion • pH • Ion-Exchange 36 BASED ON THE ORAL DRUG DELIVERY
- 37. • Nasal delivery of………….. - Organic based Pharmaceuticals - Peptide based Pharmaceuticals • Development of…………… - Epinephrine-Releasing - Hydrophilic Contact lenses 37 NASAL DRUG DELIVERY OCULAR DRUG DELIVERY NON-INVASIVE
- 38. • Transdermal delivery of………….. - Polymer Membrane Permeation - Polymer Matrix Diffusion - Drug Reservoir Gradient - Micro reservoir Dissolution • Development of…………… - Dissolution-Controlled Depot - Adsorption-type Depot - Encapsulation-type Depot - Esterification-type Depot 38 TRANSDERMAL DRUG DELIVERY PARENTAL DRUG DELIVERY
- 39. 39 RECENT TRENDS
- 40. 40 REFERENCES 1. Chien Y W; Novel Drug Delivery Systems; Informa Healthcare, 2nd Edition, 2009. 2. Siegel R A and Rathbone M J; Overview of Controlled Release Mechanisms; Advances in Delivery Science and Technology, 2012. 3. Bhowmik D, et.al; Recent trends in scope and opportunities of control release oral drug delivery systems; Critical review in pharmaceutical sciences, (1): 2012. 4. Ummadi S, Shravani B; Overview on Controlled Release Dosage Form; International Journal of Pharma Sciences, 3(4); 2013.
Editor's Notes
- #5: The term “drug delivery systems’’ refers to the technology utilized to present the drug to the desired body site for drug release and absorption.
- #7: Delivers an agent at a controlled rate for an extended time. Might localize drug action by spatial placement near where it is needed. Might target drug action by using techniques to deliver drug to a particular cell type.
- #29: In short, involves “Controlling the molecular diffusion of drug molecules in &/or across the barrier medium within or the surrounding the delivery system.”
- #33: Thereby the concentration of the triggering agent is sensed by a sensor present in the feedback-regulated type.