1
Targeted
Methods
Department of
Pharmaceutics
Faculty of Pharmacy
Kabul University
Prepared by: [Link]
2
3 Introduction and Classification
of Nanoparticles
4 Introduction
o Nanoparticles is derives from the
Greek word Nanos
• Nanos means extremely small.
5
Cont.
o NPs are solid, colloidal particles composed of natural, synthetic or semisynthetic
polymers.
o Size range: 10 - 100 nm.
o The drug is dissolved, entrapped, encapsulated or attached to a NPs matrix.
o The materials which are used for the preparation of NPs should be non- toxic,
biodegradable, sterlizable etc..
Cont.
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Polymers
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o Natural polymers
• Protein
• Albumin
• Polysaccharides
• Dextran
• Chitosan
Cont.
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o Synthetic polymers
• Polystyrene
o Semisynthetic polymers
• Cellulose derivatives
Advantages
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o Site- specific delivery of drug.
o NPs helps to achieve maximum therapeutic response with minimum adverse
effects.
o Active and passive drug targeting can be achieved by manipulating the particle
size and surface characteristics of NPs.
o NPs can be administrated by parenteral. Oral, nasal or ocular routes.
o By attaching specific ligands onto their surfaces, NPs can be used for directing
the drugs to specific target cells.
10
Disadvantages
o Small size and large surface area can be lead to particle aggregation.
o Handling of NPs difficult in liquid and dry forms.
o Limited drug loading
11 Selection of materials
Is dependent on many factors including:
1. Size of NPs required
2. Inherent properties of the drug
3. Surface characteristics such as charge and permeability
4. Degree of biodegradability, biocompatibility and toxicity
5. Drug release profile desired
6. Antigenicity of the final product.
12 Classification of NPs
1. Solid Lipid Nanoparticles(SLN)
2. Magnetic Nanoparticles(MNPS)
3. Polymeric Micelles(PMs)
4. Liposomes
5. Microcapsules
6. Microspheres
13 Preparation Methods and
Evaluation of NPs
14 Methods of Preparation
o Super critical fluid technology
o Performed polymer
• Solvent evaporation method
• Solvent displacement method
• Salting out method
Cont.
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o Polymerization Methods
• Interfacial polymerization
• Dispersion polymerization
• Emulsion polymerization
16 Evaluation
o Particle size: Is important parameter that governs stability, drug loading and
rate of drug release. It is determined by electron microscopy.
o Surface area: It is determined by spectrometer.
o Surface charge: It is measured by zeta potential.
o Density: It is determined by gas pycnometer.
Cont.
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o Molecular weight: It is determined by gel permeation chromatography.
o Nanoparticle yield: Given in term of %
o Drug entrapment efficiency: Given by equitation.
o Invitro release: It is determined by:
• Diffusion cell
• Ultra filtration
18 Application and Preparation
Methods of Liposomes
.
Introduction
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o Liposomes: Liposomes is derives from the Greek word:
• Lipo mean fat and Somes mean body.
• Size range: 50- 500 nm
• Liposomes are spherical, self- closed structures formed by one or several
concentric lipid bilayer with an aqueous phase inside.
20 Cont.
o liposomes were first proposed and tested as a drug delivery system in the early
1970s.
o Since then, they have been adopted as the vehicle choice for drug delivery and
targeting due to their very unique and attractive biological, physical and
chemical properties.
o Liposomes are biocompatible and can both entrap and protect water-soluble
molecules in their internal water compartment and water-insoluble into the
membrane.
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Composition
The main component of liposomes are:
1. Phospholipids: Phospholipids are the major structural components of
biological membranes such as the cell membrane.
• Phosphoglycerides
• Sphingolipids
2. Cholesterols: Stabilizes membrane and plays important role in bilayer formation.
Advantages
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o The ability incorporate and deliver relatively large amounts of drug.
o The possibility to decorate their surface with different ligands.
o The ability to increase both the safety and the efficacy of many drugs.
• Liposomes have been used clinically as delivery systems
23 Disadvantages
o Fast systemic elimination.
o Metabolic degradation of the phospholipids.
o Vesicle stability issue after large scale production and storage.
o Inability to provide sustained release of drugs.
• Some of these problems have been particularly overcome and marketed
liposomes of the newest generation are more stable with shelf- life up to
several months.
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Applications
o Diagnostic Application
o Therapeutic Application
25 Preparation Methods
o General Methods of Preparation
o Mechanical Dispersion Method
o Solvent Dispersion Method
o Revers Phase Evaporation Method
o Detergent Removal Method
26 Marketed Products
27 References
1. Textbook on Novel Drug Delivery System (PB 2021) Paperback – 1 January 2021.
2. A Textbook of Controlled Drug Delivery Systems: With Novel Natural Controlled
Release Polymer (Hibiscus Rosa Sinensis gum) Paperback – August 16, 2019
3. Dua K, Mehta M, Pinto TD, Pont LG, Williams KA, Rathbone M, editors. Advanced
Drug Delivery Systems in the Management of Cancer. Elsevier; 2021 Jun 24.
4. Adepu S, Ramakrishna S. Controlled drug delivery systems: current status and
future directions. Molecules. 2021 Sep 29;26(19):5905.
5. Misra A, Shahiwala A. Novel Drug Delivery Technologies. Springer:
Berlin/Heidelberg, Germany; 2019
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