A PHARMACEUTICAL NANOSUSPENSION IS DEFINED AS: “Very finely dispers solid drug particles in an aqueous vehicale for either oral and topical use or parenteral and pulmonary administration.
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nanosuspension technology by sajid
1. NANOSUSPENSION
TECHNOLOGY
Presented By:
Syed Sajid Syed Noor
Under The Guidance Of
Asst. Proff. Mr. Sandip Phoke
Shri R. D. Bhakt College of Pharmacy, Jalna
Dr. Babasaheb Ambedkar Marathwada
University, Aurangabad-431147 (MS), India
2. INTRODUCTION
A PHARMACEUTICAL NANOSUSPENSION IS DEFINED AS:
“Very finely dispers solid drug particles in an aqueous vehicale for either oral and
topical use or parenteral and pulmonary administration.
The partical size distribution of solid particals in nanosuspension is between 200 and 600 nm.
Rout of administration:-
1-oral
2- topical/ parenteral.
3- pulmonary.
3. PROPERTIES
Usually less than one micron with the average particle size ranging 200-
600nm
Drug is maintained in the required crystalline form with reduced particle size
leads to the increased dissolution rate and enhances the bioavailability
Increased insolubility and dissolution velocity
Increase in apparent saturated solubility Cs, and Surface area.
Increased dissolution velocity
increase adhesiveness.
4. Advantages of nanosuspension
technology.
1-oral rout of administration.
2-intravenus R.A.
3-S.c/I.m.rout of administration.
4-Occular/ inhalational R.A.
5-Nanosuspension technology can be encorporeted in
tablets,pellets,hydrogel,suppositories are suitable for various
rout of administration.
5. Special features.
1- increase saturation solubility.
2-increase dissolution rate of drugs.
3-increase adhesive nature and due to enhance bioavailibility.
4-possibility of surface modification of nanosuspension for site
specific delivery.
7. PREPARATION TECHNIQUES
Top - Down Approach[3]
• Wet Milling
• High Pressure Homogenization
Bottom – up Approach[3]
• Liquid Antisolvent Precipitation
• Liquid Emulsion Technique
• Sonoprecipitation
8. CHARACTERIZATION
Particle size distribution:
Determining particle size distribution are photon correlation spectroscopy (PCS), laser
diffraction (LD), dynamic light scattering (DLS) and coulter counter multisizer.[9]
Zeta Potential (Particle charge distribution):
It is determined by Zetasizer.
Nanosuspensions exhibiting good stability, for an electrostatically stabilized
Nanosuspensions a minimum zeta potential of ± 30mv is required whereas in the case
of a combined electrostatic and steric stabilization, a minimum zeta potential of ± 20mV
is desirable.[10]
10. CHARACTERIZATION
Saturation solubility and dissolution velocity:
Nanosuspensions increase the dissolution velocity and saturation solubility.
Size reduction leads to increase in the dissolution pressure.
An increase in solubility that occurs with relatively low particle size reduction may be
mainly due to a change in surface tension leading to increased saturation solubility.[1]
11. APPLICATION
Bioavailability enhancement:
Nanosuspensions resolve the problem of poor bioavailability by solving problems of poor
solubility and poor permeability across the membrane.[12]
Target drug delivery:
Nanosuspensions can also be used for targeted delivery as their surface properties and
in vivo behaviour can easily be altered by changing either the stabilizer.[12]
12. APPLICATION
Topical formulations:
Drug nanoparticles can be incorporated into creams and water-freeointments.
The nanocrystalline form leads to an increased saturation solubility of the drug in the
topical dosage form, thus enhancing the diffusion of the drug into theskin.[12]
Mucoadhesion of the nanoparticles:
Nanoparticles orally administered in the form of a suspension diffuse into the liquid
media and rapidly encounter the mucosal surface.
The particles are immobilized at the intestinal surface by an adhesion mechanism
referred to as bioadhesion.[12]
13. APPLICATION
intra-articular, intraperitoneal,
Parenteral administration:
Can be administered via different parenteral routes like
intravenous injection.
For administration by the parenteral route, the drug either has to be solubilized or has
particle/globule size below 5 μm to avoid capillary blockage.
The current approaches for parenteral delivery include salt formation, solubilization
using co-solvents, micellar solutions, complexation with cyclodextrin and recently
liposomes.[12]
Oral administration:
Nanosizing of drugs can lead to a dramatic increase in their oral absorption and
subsequent bioavailability.[12]
14. Few current marketed formulations using
nanosuspension technology.
1-Retinoic acid -to attain controlled release and high saturation
solubility of drugs.
2-acyclovir -for prolonged rełease of drug and to increase
bioavailibility.
3-itraconazole -increase aqueous solubility and dissolution and
hence increase bioavailibility.
4-Diclofenac - to enhance solubility of drug.( i.m).
5- Atorvastatin - to enhance solubility of drug .
6-Miconazole - to increase bioavailibility.
15. The maine aim of nanosuspension
technology.
- To provide the maximum therapeutic effect in minimum
periodes of time.
16. 1. Dhanapal, R., & Ratna, J. V. (2012). Nanosuspension technology in drug delivery: A Review. International journal of Pharmacy Review &
Research, (1), 46–52
2. Agrawal, U., Sharma, R., Gupta, M., & Vyas, S. P. (2014). Is nanotechnology a boon for oral drug delivery? Drug Discovery Today, 19(10),
1530–1546.
3. Chan, H.K., & Kwok, P.C. L. (2011). Production methods for nanodrug particles using the bottom-up approach. Advanced Drug Delivery
Reviews, 63(6), 406–416.
4. Itoh, K., Pongpeerapat, A., Tozuka, Y., Oguchi, T. & Yamamoto, K. (2003). Nanoparticle formation of poorly water soluble drugs from ternary ground
mixtures with PVP and SDS. Chem Pharm Bull., 51,171-4.
5. Patravale, V.B., Date, A. A. & Kulkarni, R. M. (2004). Nanosuspensions: a promising drug delivery strategy. J Pharm Pharmacol., 56,827-40.
6. Margulis-Goshen, K., & Magdassi, S. (2009). Formation of simvastatin nanoparticles from microemulsion. Nanomedicine: Nanotechnology,
Biology, and Medicine, 5(3), 274–281.
7. Addio, S. M., & Prud’homme, R. K. (2011). Controlling drug nanoparticle formation by rapid precipitation. Advanced Drug Delivery Reviews,
63(6), 417–426.
8. Jiang, T., Han, N., Zhao, B., Xie, Y., & Wang, S. (2012). Enhanced dissolution rate and oral bioavailability of simvastatin nanocrystal prepared by
sonoprecipitation. Drug Development and Industrial Pharmacy, 38(10),1230–1239.
9. Shid, R.L., Dhole, S. N., Kulkarni, N., & Shid, S. L. (2014). Formulation and Evaluation of Nanosuspension Delivery System for Simvastatin,
7(2), 205-217
10. Liang, Y.C. & Binner J.G.P. (2008). Effect of triblock copolymer non-ionic surfactants on the rheology of 3 mol% yttria stabilised zirconia
Nanosuspensions. Ceram Int., 34, 293-297.
11. Gupta, D.K., Razdan, B.K., & Bajpai, M. (2014). Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles, International journal of
pharmaceutical sciences and nanotechnology, 7(1), 2377–2386.
REFERENCE