WELCOME

ROUTES OF ADMINISTRATION OF BIOTECH PRODUCTS:

PARENTERAL ROUTES CONSIDERING NANOPARTICLES

& MICROEMULSION

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PRESENTED BY

GROUP MEMBERS REGISTRATION NO

Rachana Sarkar 12103022

Susmita Ghosh 12103023

Furhatun-Noor 12103048

Priyanka Florina Karmokar 12103050

Tajrian Rahman 12103059

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CONTENTS

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Microemulsion

– Advantages and disadvantges of microemulsion

– Classification

– Preparation

– Application

– Overview of parenteral microemulsion and their in-vivo

advantages

– Microemulsion based marketed product

CONTENTS

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BIOTECH PRODUCTS

Biotech is the term used for

biotechnology or products

produced by biotechnology.

True biotech products are

manufactured in live biological

systems known as expression

systems.

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ROUTE OF ADMINISTRATION OF BIOTECH DRUG PRODUCTS

Route of Administratio

n

Oral Parenteral Nasal Transmucosal

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PARENTERAL ROUTE OF ADMINISTRATION

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PARENTERAL DRUG DELIVERY SYSTEM OF BIOTECH PRODUCT

The drug carrier systems used for defined and controlled delivery of drug through this route can be: Particulates Soluble carriers (Macromolecules) Others

There are different types of particulate carrier systems .These are: Microspheres Microcapsules Nanoparticles Aquasomes Liposomes Emulsions

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IMPORTANCE OF PARTICULATE CARRIERS IN BIOTECH DRUG PODUCTS

Importance

Increased patient efficacy

Increased specific

localization

Decreased toxic side

effects

Reduced dose

Controlled bio

distribution

Modulated pharmacoki

netics

Improved patient

compliance

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NANOPARTICLES

Nanoparticles are the end products of a wide variety of physical, chemical and biological processes some of which are novel and radically different, others of which are quite commonplace.

Nanoparticles may be defined as submicron (<1µm) colloidal systems, generally, but not necessarily, made of polymers (biodegradable or not).

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Nanoparticles

Nanospheres (Matrix type

structure in which a drug is

dispersed)

Nanocapsules (Membrane wall structure with an

oil core containing drug)

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ADVANTAGES OF NANOPARTICLES

Can be administered by parenteral, oral, nasal, ocular routes.

By attaching specific ligands on to their surfaces, nano particles can be used for directing the drugs to specific target cells.

Improves stability and therapeutic index and reduce toxic effects.

Both active & passive drug targeting can be achieved by manipulating the particle size and surface characteristics of nano particles

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ADVANTAGES OF NANOPARTICLES

Small size & large surface area can lead to particle aggregation .

Physical handling of nano particles is difficult in liquid and dry forms.

Limited drug loading.

Toxic metabolites may form.

DISADVANTAGES OF NANOPARTICLES

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TYPES OF NANOCARRIERS

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PREPARATION OF POLYMERIC NANOPARTICLES

Preparation Methods

Polymerization Preformed Polymer

Supercritical Fluid

Technique

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Polymerization

Dispersion Polymerization

Emulsion Polymerization

PREPARATION OF POLYMERIC NANOPARTICLES

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Pref

orm

ed P

olym

erSolvent

Evaporation

Solvent Displacement

Salting out

PREPARATION OF POLYMERIC NANOPARTICLES

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APPLICATIONS OF NANOPARTICLES

Nanomedicine

Chemicals & Cosmetics Food Science Materials Electronics

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APPLICATION OF NANOPARTICLES IN MEDICINE

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SELECTED NANOPARTICLE BASED PARENTERAL THERAPEUTICS APPROVED BY FDA

AMBISONE ABRAXANE

MACGUEN SOMAVERT

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SELECTED NANOPARTICLE BASED PARENTERAL THERAPEUTICS APPROVED BY FDA

Brand Name Nanoparticle Component

Company Indication

Abraxane paclitaxel (taxol) boundalbumin nanoparticles

AbraxisBioScience

AstraZeneca

metastatic breastcancer patientswho have failed

combinationtherapy

Ambisome Amphotericin B liposomes

Gilead Sciences

Fungal infection

Macugen pegylated anti-VEGFaptamer

OSIPharmaceutical

sPfizer

neovascular age-related macular

degeneration

Somavert pegvisomant (PEG-hGH) NektarPfizer

Nacromegaly

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WHAT IS MICROEMULSION?

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MICOEMULSION is a-

Homogenous

Transparent

Thermodynamically stable

dispersion of water & oil

Stabilized by Surfactant

Co-surfactant is combined

Diameter of droplets between

100Å to1000Å.

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HISTORY & DEVELOPMENT OF MICROEMULSION

INVENTORS CONTRIBUTION YEAR

Hoar & Schulman Introduce the concept of “MICROEMULSION” by generating clear

phase solution

1943

Schulman Coined the term “ MICROEMULSION”

1959

Rodawald First commercial “MICROEMULSION” was dicovered

1928

Danielson & Lindman

Definition of MICROEMULSIONprovided 1981

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COMPARISON BETWEEN EMULSION & MICROEMULSION

Thermodynamically unstable. In due time phases it is separate

out. It is cloudy. Require large input of energy

during its preparation. higher cost.

Droplet size > 500 nm Interfacial tension: high High viscosity

MICROMULSION

Thermodynamically stable. In due time phases it is not

separate out. It is transparent. Require low input of energy

during its preparation. relatively low cost.

Droplet size 10-200 nm Interfacial tension: ultra low Low viscosity with Newtonian

behavior.

EMULSION

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COMPARISON BETWEEN EMULSION & MICROEMULSION

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ADVANTAGES OF MICROEMULSION BASED SYSTEM

Increases the rate of absorption .

Eliminates variability in absorption

Helps to solubilize lipophilic drug

Provides a aqueous dosage form for water insoluble drugs

Increases bioavailability

Various routes like topical, oral and intravenous can be

used to deliver the product

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• Rapid and efficient penetration of the drug moiety.

• Helpful in taste masking

• Provides protection from hydrolysis and oxidation

• Liquid dosage form increases patient compliance.

• Less amount of energy requirement.

ADVANTAGES OF MICROEMULSION BASED SYSTEM

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Large concentration of surfactant and co-surfactant are required.

Limited solubilizing capacity for high-melting substances.

The surfactant must be nontoxic for using pharmaceutical

applications.

Microemulsion stability is influenced by environmental

parameters.

DISADVANTAGES OF MICROEMULSION BASED SYSTEM

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CLASSIFICATION OF MICROEMULSION

• With two phases , the lower

• o/w type

Winsor I

• With two phases, the upper

• w/o type

Winsor II• With

three phases, the middle

• o/w+w/o type

Winsor III

• In a Single phase, with oil, water & surfactant

Winsor IV

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CLASSIFICATION OF MICROEMULSION

Types of Microemulsion

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COMPONENTS OF MICROEMULSION

Aqueous Phase

• Water

Oil Phase

• Isopropyl Myristate

• Mineral oil

• Olive oil• Oleic acid

Surfactant

• Tween 80• Tween 40• Span 40• Lecithin

Co-surfactant

• PEG 400• Propylene

glycol• Ethylene

glycol• Glycerol

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PREPARATION OF MICROEMULSION

Preparation Method of

Microemulsion

Phase Titration Method

Phase Inversion Method

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PHASE TITRATION METHOD

Aqueous Phase Titration Method

Oil+Surfactant+Co-surfactant

Titration with water

Stirring

Clear dispersion

Microemulsion

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PHASE INVERSION METHOD

Carried out upon addition of excess of the dispersed phase

or in response to temperature.

Drastic physical changes occur.

Water droplet added to oil phase

Stabilizing o/w to w/o microemulsion

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APPLICATIONS OF MICROEMULSION

Microemulsion

Drug Delivery System

Biotechnology

Cosmetics

PharmaceuticalsAgrochemicals

Food Science

Others

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MICROEMULSION IN DRUG DELIVERY SYSTEMS

Applications

Parenteral Administration.

Oral drug delivery.

Topical drug delivery.

Ocular and pulmonary

delivery.

Micro-emulsions in

biotechnology

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OVERVIEW OF PARENTERAL MICROEMULSION AND THEIR IN-VIVO ADVANTAGES

DRUG NAME IN-VIVO ADVANTAGE

Paclitaxel Less hypersensitivity reaction, higher AUC value and prolonged circulation as compared with Taxol

Flurbiprofen Prolonged circulation and higher AUC values as compared with the solution

Clonixic acid Less painful as compared with marketed formulation

Vincristine Higher efficacy, survival rate and lesser side effects as compared with free drug

Ibuprofen Prolonged circulation and higher AUC values as compared with the solution.Source: Katiyar et al., 2013

Source: (Nagarsenkar et al., 2008).Source: (Nagarsenkar et al., 2008).

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MICROEMULSION BASED MARKETED PRODUCT

Brand Name Composition Manufacturer

Sandimmune Neoral® Cyclosporin A Novartis

Norvir ® Ritonavir Roche laboratories

Fortovase ® Saquinavir Roche laboratories

White Glow Mulberry Extract Lotus Herbals

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Enhancing the efficacy of existing of drug is an ongoing process in

pharmaceutical research.

Multiferous materials and principles have been employed to generate

polymer-based particulate systems and rigid, semi-rigid and vescicular

lipoidal colloid drug delivery vehicles.

Microemulsion has achieved a favorable position because of their non

particulate nature, components of bio-origin and provisions for

modifications in the constructs so that they can be tailored to suit the

target site.

CONCLUSION

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REFERENCE

• Bhowmik D, Harish.GB, Kumar, Aravind G. MICROEMULSIFYING DRUG DELIVERY

SYSTEM-NEW ERA OF DRUG DELIVERY SYSTEM. Indian Journal of Research in

Pharmacy and Biotechnology, 2013; 1(1): 47.

• Ghosh PK, Murthy RS, “Microemulsions: A potential drug delivery system”, Current

Drug Delivery, 3(2), 2006, 167-180.

• Jha SK, Dey S, Karki R. Microemulsions- Potential Carrier for Improved Drug

Delivery. Asian Journal of Biomedical and Pharmaceutical Sciences, 2011; 1 (1): 5-9.

• Katiyar BS, Katiyar SS, Mishra PS, Sailaja DL. Microemulsions: A Novel Drug Carrier

System. International Journal of Pharmaceutical Sciences Review and Research, May

– Jun 2013; 20(2): 138-148.

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