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PREPARED BY GUIDED BY

Dimendra Patel Dr. Nazneen Surti

Department of Pharmaceutics

Baroda college of pharmacy

Limda - vadodara

SOLID LIPID NANOPARTICLES

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INTRODUCTION

New approach to deliver lipophilic drug

It is same as an oil in water emulsion for parenteral nutrition, but

the liquid lipid of the emulsion has been replaced by solid lipid

Resulting in the formation of SLN having size range of 100-

150nm.

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The system consists of spherical solid lipid particles in thenanometer range, dispersed in water or in aqueous surfactant

solution.

They have ability to carry lipophilic or hydrophilic drugs ordiagnostics.

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Why Solid Lipid Particle ???

40% of lipophilic drug candidates fail because

Their solubility and

Formulation stability problem

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MERITS:-

Good biocompatibility

Non toxic

Stable against Hydrolysis

Biodegradable

Physically stable

Good carrier for lipophillic drugs

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Advantages and Disadvantages of various

colloidal drug carrier systems

Sr

.

N

o.PROPERTY SLN POLYMER

NANOPARTICLES LIPOSOMES LIPIDEMULSIONS

1

Systemic toxicity

Low

> or = to SLN

Low

Low

2 Cytotoxicity Low > = to SLN Low Low3 Residues from organic

solvents No Yes May or may not No

4 Large scale production Yes No Yes Yes5 Sterilization by autoclaving Yes No No Yes6 Sustained release Yes Yes < or = to SLN No

7 Avoidance of RES Depend onsize andcoating

No Yes Yes

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General ingredients:- Solid lipid

Triglycerides (e.g. tristearine, hard fat)Partial glycerides (e.g. Imwitor)

Pegylated lipids,

Fatty acids (stearic acid)

Steroids (e.g. cholesterol)

Waxes (e.g. cetylpalmitate)

Emulsifier

All classes of emulsifiers have been used to stabilize the lipid dispersion.

Example :- poloxamer, polysorbates, lecithin and bile acids

Water

As a aqueous phase

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PREPARATION METHODS:-

High pressure homogenization

Microemulsification- solidification technique

Multiple microemulsion- solidification technique

Ultra sonication or high speed homogenization

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SLNs preparation using supercritical fluid

SLNs prepared by solvent emulsification/evaporation

Spray drying method

Double emulsion method

PREPARATIONMETHODS.

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1. HIGH PRESSURE HOMOGENIZATION (HPH)

High pressure homogenizers push a liquid with high pressure (100-2000 bar) through a narrow gap

(in the range of few microns).

The fluid accelerates on a very short distance to very high

velocities.

The high shear stress disrupts the particles down to the submicron

range.

Two type

HOT HOMOGENIZATION TECHNIQUE

COLD HOMOGENIZATION TECHNIQUE

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HOT HOMOGENIZATION TECHNIQUE

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USE:-

LipophilicInsoluble drugs

Not suitable for incorporation of

Hydrophilic drugs &

Heat Sensitive Drug

PROBLEMS:-

(1) Temperature induced drug degradation(2) Drug distribution into the aqueous phase during homogenization

(3) Complexity of the crystallization step of the nanoemulsion

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COLD HOMOGENIZATION TECHNIQUE

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USE:-

Hydrophilic drugs

Thermosensitive

Thermolabile drugs.

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2. MICROEMULSIFICATION- SOLIDIFICATION TECHNIQUE

Melting of lipid

Preparation of microemulsion by dispersing melted lipid in aqueous

medium containing drug under mechanical stirring at 65-70 oC

Rapid crystallization of oil droplet on dispersion in cold medium

Solid lipid nanoparticles

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3. MULTIPLE MICROEMULSION- SOLIDIFICATION

Melting of lipidAdd aqueous solution of drug to melted lipid

Add Surfactant and co-surfactant at a temperature above the melting point of lipidFormation of clear w/o microemulsion

Formed w/o microemulsion is added to a mixture of water, surfactant

and co-surfactant under mechanical stirringFormation of suspension of lipid particles

Wash with dispersion medium by ultrafiltration system

Solid lipid nanoparticles

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Other Technique

Ultra sonication or high speed homogenization

SLNs preparation using supercritical fluid

SLNs prepared by solvent emulsification/evaporation

Spray drying method

Double emulsion method

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CHARACTERIZATION OF SLNs:-

1. PARTICLE SIZE AND SHAPE

2. PARTICLE CHARGE

3. STRUCTURE

4. DETERMINATION OF INCORPORATED DRUG

5. IN-VITRO DRUG RELEASE STUDIES

6. RHEOLOGY

7. STORAGE STABILITY

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ADVANTAGES :-

1. High drug levels can be achieved at the site of disease and systemic side

effects can be reduced..

2. Controlling the release profile..

3. SLN formulation can remain stable for even the years..

4. Suitable for both hydrophilic and hydrophobic drugs..

5. Drugs can be protected against chemical degradation by solid matrix of SLN..

6. Large scale production and sterilization is possible..

7. SLNs is prepared from physiological lipid which decreases the risk of acute

and chronic toxicity..

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DISADVANTAGE:-

Poor drug loading capacity.

During storage, drug expulsion after polymeric

transition.

Water content of the dispersions is relatively high (70-

99.9%).

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APPLICATION:-

1. TOPICAL GLUCOCORTICOIDS

2. ANTIANDROGEN

3. SLNs FOR TOPICAL USE

4. ORAL SLNs IN ANTITUBERCULAR CHEMOTHERAPY

5. SLNs AS COSMECEUTICALS

6. SLNs AS GENE VECTOR CARRIER

7. SLNs IN BREAST CANCER AND LYMPH NODE METASTASES

8. SLNs AS A TARGETED CARRIER FOR ANTICANCER DRUG TO SOLID TUMORS

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PRODUCT NAME PRODUCER

Cutanova Cream Nano Repair Q10

Intensive Serum NanoRepair Q10

Cutanova Cream NanoVital Q10

Dr. Rimpler

SURMER Crme Legre Nano-Protection

SURMER Crme Riche Nano-Restructurante

SURMER Elixir du Beaut Nano-Vitalisant

SURMER Masque Crme Nano-Hydratant

Isabelle Lancray

NanoLipid Restore CLR Chemisches Laboratorium

Nanolipid Q10 CLR

Nanolipid Basic CLR

NanoLipid Repair CLR

Dr. Kurt Richter, (CLR)

Examples of cosmetic products currently on the market containing lipid

nanoparticles.

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CONCLUSION:-

Drug molecules into the target site in a controlled manner.

Minimizing the problems related to solubility, permeability and

toxicity that are associated with the respective drug molecules.

High physical stability .

Incorporating both the lipophilic and hydrophilic drug molecules

makes the SLNs drug delivery system more promising.

SLNs Useful for variety of drug molecules including analgesics,antitubercular, anticancer, vitamins, steroids and anti inflammatory

agents to the target site.

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REFERENCES:-

Nanoparticulates as drug carriers , Published by Imperial College Press . Solid

Lipid Nanoparticles . 217 243

http://en.wikipedia.org/wiki/Solid_lipid_nanoparticle

Westesen K, Bunjes H, Do nanoparticles prepared from lipid solid at room

temperature always possess a solid lipid matrix? Int. J. Pharm.115 (1995),

62-69. Mller RH. Mehnert W., Souto EB., 2005. Solid lipid nanoparticles (SLN) and

nanostructured lipid carriers (NLC) for dermal delivery. In: Bronaugh, R.L. (Ed.),

Percutaneous Absorption, 4th ed, pp. 719738.

Eldem T, Speiser P, Hincal A. Optimization of spray-dried and congealed lipid

microparticles and characterization of their surface morphology by scanning

electron microscopy. Pharm Res 1991; 8:47-54.

http://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticlehttp://en.wikipedia.org/wiki/Solid_lipid_nanoparticle

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THANK YOU.