Suyesh V.Kale: S.S.D.J. College of Pharmacy, Chandwad

PRESENTED BY
Suyesh V.Kale
M. PHARM Ist Year
(PHARMACEUTICS)
S.S.D.J. COLLEGE OF PHARMACY, CHANDWAD.
Introduction Properties Formulation aspects Post production techniques Characterization Applications References
CONTENTS
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S.S.D.J. College of Pharmacy,Chandwad. December 13, 2012
Introduction
More than 40 % NCEs are Brick or Grease ball candidates. Possess formulation as well as other problems.
Lowering the particle size serves a standout approach.

A highly advantageous technique.
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Definition
Nanosuspensions can be defined as colloidal dispersions of drug particles that are produced by a suitable method and are stabilized by a suitable stabilizer.
A pharmaceutical nanosuspension is defined as very finely dispersed drug particles in an aqueous drug vehicle.
Particle size is generally between 200-600 nm.
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Increase in dissolution solubility
Ease of scale up
Ease of manufacture
Long term physical stability
For poorly water soluble drugs
Increase in saturation solubility
Versatility
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Nanosuspensions
Top down technology

Melt emulsification
Bottom up technology Nanopure Nanojet Supercritical fluid method
High pressure homogenization Microfluidization Precipitation combined high pressure homogenization Media milling Microemulsion template 6
December 13, 2012
S.S.D.J. College of Pharmacy,Chandwad.
High Pressure Homogenization
High pressure plunger pump
Relief valve or homogenizing valve
HPH
1. Use to prepare poorly soluble drugs. 2.Suspension of drug and surfactant is forced under reduced pressure. 3.e.g. DISSOCUBES, R.H.Muller it is also known as piston gap technology.
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Advantages Disadvantages Equipment: APV Micron Lab 40. Actual mechanics Various types of instruments available
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High pressure homogenization
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Microfluidization
Coarse suspension of drug stabilizer and dispersion medium are added
Passed through chamber
Breakage of suspension nanosuspension Production parameters affecting it
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Microfluidization
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Precipitation combined high pressure homogenization

Works on the same principle as that of high pressure homogenization. Use of high energy process to form crystalline particles. Need of forming a presuspension of the drug.
Nanopure technology
Specially used for chemically labile drugs
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Nanoedge technology
Specially used for friable materials. Owned by Baxter corp. Precipitated dispersion is further precipitated to get smaller particle size. Water miscible solvents like ethanol, methanol, isopropanol.
Nanojet technology
Stream of suspension in two or more parts were passed under high pressure resulting in reduction in particle size.
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Nanoedge technology
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Microemulsion template
For drugs soluble in organic solvents

Organic solvent and drug surfactants
Evaporation of organic phase under reduced pressure

Coating of drug in internal phase Formation of microemulsion
Diluting the microemulsion

Advantages Disadvantages
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Partially water miscible solvents
HPH
Nan osuspension
Formation of emulsion
Dilution
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Use organic solvent dissolve drug in internal phase
Formation of crude emulsion
High pressure homogenization

nanosuspension
Alternatively hydrosol technology is also used

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Media milling technology
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Wet Media milling technology
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Melt emulsification method
Drug and stabilizer
Heat above M.P. of drug
Homogenization
Cool emulsion on ice bath
Maintain temp. of emulsion above M.P. of drug
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Supercritical method
Safer as compared to other methods. Most commonly used techniques are: 1. Supercritical antisolvent (SAS) 2. Precipitation with compressed antisolvent process ( PCS ) 3. Rapid expansion of supercritical solution ( RESS )
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Microprecipitation or Controlled Precipitation

Here rapid addition of drug to antisolvent is there. Further supersaturation leads to formation of ultrafine amorphous drug solids. Two phases: nuclei formation and crystal growth Ratio of mixing time to precipitaion time is important.
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Microprecipitation or Controlled Precipitation
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Dry co grinding method
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Other technologies
1. Acid base neutralization 2. High gravity reactive precipitation technique. 3. Precipitation ultrasonication 4. Solvent displacement method.
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Properties of nanosuspension
Saturation solubilty Change of state Absence of ostwald ripening Noyes Whitney equation
Adhesivenes
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Properties of nanosuspension
Noyes-Whitney equation dx/dt = [( D x A/ h] [Cs-X/V] Where D is diffusion coefficient A is surface area of particle V is volume of dissolution medium X is the concentration in surrounding liquid h is the diffusional distance dx/dt is the dissolution velocity Cs is the saturation solubility of the drug
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Formulation aspects of nanosuspension

1. Addition of stabilizer : to prevent ostwalds ripening and agglomeration Since high surface energy present in nanoparticles. 2. In some cases mix. Of stabilizer is needed. e.g. cellulosics, ploxamer, polysorbates, lecithins, an povidones
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Formulation aspects of nanosuspension

2. Use of organic solvents: Specially for microemulsion templates. E.g. ethanol and isopropanol, ethyl acetate, triacetin, benzyl alcohol. 3. Co-surfactants : used for microemulsion type of methods 4. Other additives : buffers, salts, polyols, cryoprotectant.
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Evaluation of nanosuspension
Mean particle size and distribution: Polydispersibility index- measured by using laser diffractometry, AFM, PCS, Coulter counter technique. Particle charge ( Zeta potential ) Using zetasizer.
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Crystalline state and particle morphology. Determined by use of XRD, DSC and wide angle X-ray analysis (WAXS) Saturation solubility and dissolution velocity. pH Osmolarity Drug content Stability study: using Malvern mastersizer. Evaluation of surface modification Done by using 2 D PAGE and HIC
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post production of nanosuspension
1) 2) 3) 4)
Solidification techniques : Mainly used to due to concerns like ostwalds ripening an agglomeration Includes processes like pelletization, granulation, spray drying, lyophilization Improves redispersibility of particles. Addition of matrix formers may be needed e.g. avicel, aerosil. Surface modification techniques: sometimes burst release or passive targeting is there. hence need of surface modification techniques
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S.S.D.J. College of Pharmacy,Chandwad.
December 13, 2012
Post Production of nanosuspension
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Post Production of nanosuspension
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Applications
Parenteral administration: Nanosuspensions can be administered via different parenteral administration routes ranging from intra-articular via intraperitonal to intravenous injection. the drug either has to be solubilized or has particle/globule size below 5 m to avoid capillary blockage. Paclitaxel nanosuspensions revealed their superiority over taxol in reducing the median tumour burden
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Applications
Ocular administration: for drugs that exhibit poor solubility in lachrymal fluids. Suspensions offer advantages such as prolonged residence time in a cul-de-sac, which is desirable for most ocular diseases for effective treatment and avoidance of high tonicity created by water soluble drugs. polymeric nanosuspension of Ibuprofen Pulmonary Drug Delivery: Aqueous nanosuspensions can be nebulized using mechanical or ultrasonic nebulizers for lung delivery Budesonide, a poorly water-soluble corticosteroid, has been successfully prepared as a nanosuspension for pulmonary delivery
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Applications
Target Drug Delivery: The engineering of stealth nanosuspensions by using various surface coatings for active or passive targeting of the desired site is the future of targeted drug delivery systems. Targeting of Cryptosporidium parvum, the organism responsible for cryptosporidiosis was achieved by using surface modified mucoadhesive nanosuspensions of bupravaquone Topical Formulations:
Drug nanoparticles can be incorporated into creams and water-free ointments.

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Marketed products
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Marketed products
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Conclusion
Nanosuspensions appear to be a unique and yet commercially viable approach to combating problems such as poor bioavailability that are associated with the delivery of hydrophobic drugs, including those that are poorly soluble in aqueous as well as organic media. Production techniques such as media milling and highpressure homogenization have been successfully employed for large-scale production of nanosuspensions. Further investigation in this regard is still essential The applications of nanosuspensions in parenteral and oral routes have been very well investigated and applications in pulmonary and ocular delivery have been realized. However, their applications in buccal, nasal and delivery are still awaiting exploration.
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References
Patel.M. and Shah.A; 2011, Nano Suspension: A novel approach for drug delivery system,Journal of Pharmaceutical Science and Bioscientific Research, 1 (1):1-10 Muller.H. and Jacobs.C., 2001, Nanosuspensions as particulate drug formulations in therapy :Rationale for development and what we can expect for the future, Advanced Drug Delivery Reviews, 47, 319. Lakshmi.P. and kumar.G., 2010, Nanosuspension technology: a review, International Journal of Pharmacy and Pharmaceutical Sciences,2(4) ; 36-40. Nayak.S. and Panda.D. , 2010, Nanosuspension:A novel drug delivery system Journal of Pharmacy Research, 3(2): 241-246. 46
References
Chingunpituk.J, 2007, Nanosuspension Technology for Drug Delivery, Walailak J Sci & Tech, 4(2): 139-153.
Patravale .V and Date.A.,2004, Nanosuspensions: a promising drug delivery strategy,journal of pharmacy and pharmacology, 56: 827840. Liu.Y. and Xie.P., 2012A mini review of nanosuspensions development, Journal of Drug Targeting, 20(3): 209223. Xiaohui.P. and Sun.J, 2009Formulation of Nanosuspensions as a New Approach for the Delivery of Poorly Soluble Drugs,
Current Nanoscience, 5, 417-427
47
Be the change you want to see in the world
48 S.S.D.J. College of Pharmacy,Chandwad. December 13, 2012
49
9 april 2012 S.S.D.J. College of Pharmacy,Chandwad.

Suyesh V.Kale: S.S.D.J. College of Pharmacy, Chandwad

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PRESENTED BY

S.S.D.J. COLLEGE OF PHARMACY, CHANDWAD.

Lowering the particle size serves a standout approach.

Increase in dissolution solubility

Long term physical stability

For poorly water soluble drugs

Increase in saturation solubility

Top down technology

Bottom up technology Nanopure Nanojet Supercritical fluid method

S.S.D.J. College of Pharmacy,Chandwad.

High Pressure Homogenization

High pressure plunger pump

Relief valve or homogenizing valve

High Pressure Homogenization

High Pressure Homogenization

High Pressure Homogenization

High pressure homogenization

Passed through chamber

Breakage of suspension nanosuspension Production parameters affecting it

Precipitation combined high pressure homogenization

For drugs soluble in organic solvents

Evaporation of organic phase under reduced pressure

Diluting the microemulsion

Partially water miscible solvents

Formation of crude emulsion

High pressure homogenization

Alternatively hydrosol technology is also used

Media milling technology

Wet Media milling technology

Wet Media milling technology

Wet Media milling technology

Melt emulsification method

Drug and stabilizer

Heat above M.P. of drug

Cool emulsion on ice bath

Maintain temp. of emulsion above M.P. of drug

Microprecipitation or Controlled Precipitation

Microprecipitation or Controlled Precipitation

Dry co grinding method

Formulation aspects of nanosuspension

Formulation aspects of nanosuspension

post production of nanosuspension

S.S.D.J. College of Pharmacy,Chandwad.

December 13, 2012

Post Production of nanosuspension

Post Production of nanosuspension

Drug nanoparticles can be incorporated into creams and water-free ointments.

Current Nanoscience, 5, 417-427

Be the change you want to see in the world

48 S.S.D.J. College of Pharmacy,Chandwad. December 13, 2012

9 april 2012 S.S.D.J. College of Pharmacy,Chandwad.

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