A Descriptive and illustrative presentation on Polymeric nanoparticles. Master of pharmacy in Pharmaceutics.

1. SEMINAR ON
PREPARATION
AND
EVALUATION OF
POLYMERIC
NANOPARTICLES

2. POLYMERIC NANOPARTICLES
 The polymeric nanoparticles (PNPs) are prepared from biocompatible and biodegradable
polymers in size between 10-1000 nm where the drug is dissolved, entrapped, encapsulated
or attached to a nanoparticle matrix.
 Depending upon the method of nanoparticles preparation, nanospheres or nanocapsules can
be obtained. Polymer-based nanoparticles effectively carry drugs, proteins, and DNA to target
cells and organs. [1]

3. Nanocapsules are systems in which the drug is
confined to a cavity surrounded by a unique polymer
Nanospheres are matrix-systems in which the
drug is physically and uniformly dispersed. [1][2]

4. ADVANTAGES DISADVANTAGES
 Increases the stability of any volatile
pharmaceutical agents, easily and cheaply
fabricated in large quantities by a multitude
of methods.
 They offer a significant improvement over
traditional oral and intravenous methods of
administration in terms of efficiency and
effectiveness.
 Delivers a higher concentration of
pharmaceutical agent to a desired location.
 The choice of polymer and the ability to
modify drug release from polymeric
nanoparticles have made them ideal
candidates for cancer therapy, delivery of
vaccines, contraceptives and delivery of
targeted antibiotics.
 Polymeric nanoparticles can be easily
incorporated into other activities related to
drug delivery, such as tissue engineering. [3]
 Limited targeting Ability
 Termination of Therapy is not possible easily.
 Might cause Cytotoxicity
 Pulmonary Inflammation and Pulmonary
Carcinogenicity.

5. HOW TO PREPARE POLYMERIC NANOPARTICLES?
POLYMERIC NANOPARTICLES PRODUCTION TECHNIQUES
NANOSPHERES Solvent Evaporation
Emulsification/Solvent Diffusion
Nanoprecipitation
Emulsification/Reverse Salting Out
NANOCAPSULES Nanoprecipitation
Depending on the type of drug to be loaded in the polymeric PNPs and their
requirements for a particular administration route, different methods can be
used for the production of the particles.[3]
In general, two main strategies are employed-
1. the dispersion of preformed polymers
2. the polymerization of monomers

6. TECHNIQUE-1 : SOLVENT EVAPORATION

7. TECHNIQUE-2 : EMULSIFICATION/SOLVENT DIFFUSION

8. TECHNIQUE-3 : NANOPRECIPITATION

9. TECHNIQUE-4 :EMULSIFICATION/REVERSE SALTING OUT

10. Preparation of Polymeric Nanoparticles can be also be done in two ways. In the schematic diagram below we
see the methods – (A) Single Emulsion and (B) Double Emulsion.

11. POLYMERS USED IN PREPARATION OF POLYMERIC NANOPARTICLES

12. EVALUATION OF POLYMERIC NANOPARTICLES
Various Evaluation Parameters that can be incorporated to characterize and evaluate
the properties and efficacy of these Nanoparticles are:-
1) Morphology :- To determine the size and shape of the nanoparticles Scanning
Electron Microscopy(SEM) is used. It can differentiate between nanospheres and
Nanocapsules.
2) Particle Size Distribution:- Along with SEM, TEM(Transmission Electron
and AFM(Atomic Force Microscopy) are used as it shows the 3D structure of
molecules.
3) Chemical Composition and Crystal Structure :- Chemical Composition is
determined by Atomic Absorption Spectroscopy, which is based on the principle of
atomic absorption, where ground state electrons of the atoms jump to an excited
state by absorbing a certain quantity of energy from light at a specific wavelength.
And Crystal Structure is determined using Time-Of-Flight mass spectrometry

13. EVALUATION OF POLYMERIC NANOPARTICLES
4) Surface Area:- . The direct measurement of the nanoparticle’s surface area uses
adsorption of an inert gas (such as N2) under varying conditions of pressure to form
a monolayer of gas coverage. The number of gas molecules that is necessary to
form a monolayer and the cross-sectional area of the adsorbate gas molecule is
related to the “total surface area”.
5) Zeta Potential:- The zeta potential (ζ) reflects the surface charge of the particles,
which is influenced by changes in the interface with the dispersing medium, due to
the dissociation of functional groups on the particle’s surface i.e; outside the
electrical double layer present above the stern layer. The zeta potential is measured
via the Zetasizer instrument. The determination of zeta potential is important for
assessing the flocculation.[4][6]

14. EVALUATION OF POLYMERIC NANOPARTICLES
6) Determination of the Drug Association:- . A widely used separation
technique is ultracentrifugation, in which the free drug, present in the
suspension, is determined in the supernatant after centrifugation. The total
drug concentration is usually determined by the complete dissolution of a
fraction of the nanoparticles in a suitable solvent. [5]
7) Determination of Drug Loading and Encapsulation Efficiency:- The free
drug and nanoparticles are separated through centrifugal ultrafiltration. The
filtrate containing solely free drug is collected for HPLC assay, while the
concentrate was freeze-dried. The freeze-dried powders are weighed and
dissolved in an organic solvent for HPLC assay of the drug content in the
nanoparticle.[7]

15. EVALUATION OF POLYMERIC NANOPARTICLES
8) In-Vitro Release Kinetics:- The release of drugs from polymeric NPs
depends on :- a) The polymeric matrix erosion,
b) the diffusion of the drug through the
polymeric wall of the nanocapsules.
USP apparatus II (Paddle) with 900 mL release medium. The sink condition
was maintained throughout the release studies.
The kinetics of drug release from nanospheres is generally in the form of an
exponential (first order), possibly due to the drug diffusion from the
polymeric matrix to the environment and/or erosion of the polymeric matrix,
releasing the drug. [5][7].
First Order Kinetics: First order kinetics refers to chemical reactions whose
rate of reaction depends on the molar concentration of one reactant.

16. CONCLUSION
 PNPs are promising vehicles for drug delivery because of easy manipulation
to prepare carriers.
 The objective of delivering the drugs to specific target can be fulfilled.
 This advantage improves the drug safety and stability.
 Can deliver a higher concentration of drug to a desired location.
 PNPs can be modified based on the type, action and location of the desired
place.

17. REFERENCES
1. Vauthier, C., Bouchemal, K. Methods for the Preparation and Manufacture of Polymeric Nanoparticles. Pharm Res 26,
1025–1058 (2009). https://doi.org/10.1007/s11095-008-9800-3
2. Zhang, G., Niu, A., Peng, S., Jiang, M., Tu, Y., Li, M., & Wu, C. (2001). Formation of Novel Polymeric Nanoparticles.
Accounts of Chemical Research, 34(3), 249–256. doi:10.1021/ar000011x
3. Soppimath, K.S.; Aminabhavi, T.M.; Kulkarni, A.R.; Rudzinski, W.E. Biodegradable polymeric nanoparticles as drug
delivery devices. J. Control. Release 2001, 70, 1–20.
4. Cano, A.; Sánchez-López, E.; Ettcheto, M.; López-Machado, A.; Espina, M.; Souto, E.B.; Galindo, R.; Camins, A.; García,
M.L.; Turowski, P. Current advances in the development of novel polymeric nanoparticles for the treatment of
neurodegenerative diseases. Nanomed. (Future Med.) 2020.
5. Sanchez-Lopez, E.; Ettcheto, M.; Egea, M.A.; Espina, M.; Cano, A.; Calpena, A.C.; Camins, A.; Carmona, N.; Silva, A.M.;
Souto, E.B.; et al. Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: In vitro and in vivo
characterization. J. Nanobiotechnol. 2018, 16, 32.
6. Martinez Rivas, C.J.; Tarhini, M.; Badri, W.; Miladi, K.; Greige-Gerges, H.; Nazari, Q.A.; Galindo Rodriguez, S.A.; Roman,
R.A.; Fessi, H.; Elaissari, A. Nanoprecipitation process: From encapsulation to drug delivery. Int. J. Pharm. 2017, 532,
66–81.
7. Weng, Jingwen & Tong, Henry & Chow, Shing. (2020). In Vitro Release Study of the Polymeric Drug Nanoparticles:
Development and Validation of a Novel Method. Pharmaceutics. 12. 732. 10.3390/pharmaceutics12080732.