Polysorbate 80 surface modified PLGA nanoparticles: an in-vitro evaluation of cellular uptake and cytotoxicity on neuro-2a cells

Abstract

Aim

Present study focuses on the development of P80 coated PLGA Nanoparticles loaded with drugs, paroxetine (P80-Par-PLGA-NPs) and clonidine (P80-CLD-PLGA-NPs) for in-vitro evaluation of Cellular Uptake & Cytotoxicity on Neuro-2a cells.

Method

P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs were developed and characterised for zeta size, potential, PDI, EE%, DL%, TEM, SEM, FTIR, DSC, in-vitro release, cytotoxicity, histopathological and cell uptake studies using rhodamine loaded P80-NPs.

Result

Mean particle diameter of P80-Par-PLGA-NPs and P80-CLD-PLGA-NPs was 204; 182.7 nm, ZP of −21.8; −18.72 mV and 0.275; 0.341 PDI, respectively. TEM and SEM images revealed homogenous surface morphology. In-vitro drug release showed sustained and complete release in 72 h. Cell viability (>90%) at C_max and no cytotoxicity in histopathology was observed. Significant higher uptake (96.9%) of P80-modified-NPS was observed as compared to unmodified-NPs (81%) (p < 0.05).

Conclusion

The finding clearly indicated a higher cell uptake of drugs via surface modified P80-coated PLGA-NPs as compared to unmodified particles.

Keywords:

• Surface modification
• cellular uptake
• polysorbate 80
• nanoparticles
• depression
• ADHD

Acknowledgement

The authors would like to thanks Jaypee Institute of Information & Technology, Noida for providing support to perform the studies and experiments.

Ethical approval

Not Applicable. The research doesn’t involve animal or human subject.

Consent to publish

All authors have provided consent for publication.

Authors’ contribution

Surbhi Sharma: conceptualisation, validation, methodology and writing the original draft, editing. Shweta Dang: conceptualisation, validation, formal analysis, investigation, review and editing.

Corresponding author: Shweta Dang

Disclosure statement

No potential conflict of interest was reported by the author(s).

Data availability statement

Not Applicable

Data deposition

Not Applicable

Notes

1 (a) Rhodamine 123 treated cells

(b) Rhodamine 123 loaded PLGA NPs treated cells

(c) Rhodamine 123 loaded Polysorbate 80 coated PLGA NPs (2 h)

(d) Rhodamine 123 loaded Polysorbate 80 coated PLGA NPs (4 h)

2 (a) Unstained Neuro-2a Cells

(b) Rhodamine 123 treated Neuro-2a cells

(c) Rhodamine 123 loaded PLGA NPs treated Neuro-2acells

(d) Rhodamine 123 loaded Polysorbate 80 coated PLGA NPs treated Neuro-2a

3 Par (Paroxetine), P80 (Polysorbate 80), P80-Par-PLGA-NPs (Polysorbate80 coated PLGA NPs loaded with paroxetine)

4 CLD (Clonidine), P80 (Polysorbate 80), P80-CLD-PLGA-NPs (Polysorbate80 coated PLGA NPs loaded with Clonidine)

5 Par (Paroxetine), P80-Par-PLGA-NPs (Polysorbate80 coated PLGA NPs loaded with paroxetine)

6 CLD (Clonidine), P80-CLD-PLGA-NPs (Polysorbate80 coated PLGA NPs loaded with Clonidine)

7 Par-PLGA-NPs (Paroxetine loaded PLGA NPs), P80-Par-PLGA-NPs (Polysorbate 80 coated PLGA NPs loaded with paroxetine), PBS (Phosphate Buffer Saline), SNF (Simulated Nasal Fluid)

8 CLD-PLGA-NPs (Clonidine loaded PLGA NPs) P80-CLD-PLGA-NPs (Polysorbate 80 coated PLGA NPs loaded with clonidine)

9 Aq drug (Paroxetine suspension), Placebo (PLGA NPs), Par-PLGA NPs (Paroxetine loaded PLGA NPs), P80-Par-PLGA-NPs (Polysorbate 80 coated PLGA NPs loaded with paroxetine).

10 Aq drug (Clonidine suspension), Placebo (PLGA NPs), CLD-PLGA NPs (Clonidine loaded PLGA NPs), P80-CLD-PLGA-NPs (Polysorbate 80 coated PLGA NPs loaded with clonidine)

C_max (Maximum concentration)

11 a Isopropyl alcohol (+ve control) treated

b P80-Par-PLGA-NPs treated

c P80-CLD-PLGA-NPs treated

d PBS (Phosphate Buffer Saline) Treated (-ve Control)

12 Encapsulation Efficiency percentage

13 Drug Loading percentage

14 Polysorbate 80 coated PLGA NPs loaded with paroxetine

15 Polysorbate 80 coated PLGA NPs loaded with clonidine

16 Encapsulation Efficiency percentage

17 Drug Loading percentage

18 Polysorbate 80 coated PLGA NPs loaded with paroxetine

19 Polysorbate 80 coated PLGA NPs loaded with clonidine

Additional information

Funding

The authors declare that no funds, grants, or other support were received during the preparation of this manuscript.