SELF-ASSEMBLED CHITOSAN NANOPARTICLES FOR PERCUTANEOUS DELIVERY OF CAFFEINE: PREPARATION, CHARACTERIZATION AND IN VITRO RELEASE STUDIES


Nik Amanina Farhanah Abu Hassan, Shariza Sahudin, Zahid Hussain, Mumtaz Hussain, Mumtaz Hussain

Abstract


Objective: Chitosan (CS)–tripolyphosphate (TPP)–nanoparticles (NPs) have been extensively studied during the past few decades due to their well-recognized applicability in various fields. The present study attempts to optimise the development of these nanoparticles to enhance the percutaneous delivery of caffeine.

Methods: CS-TPP-NPs were prepared via ionic cross-linking of CS and TPP and were characterized. The influence of several formulation conditions (CS: TPP mass ratio and concentration of caffeine) and process parameters (stirring speed, stirring time and ultra-sonication time) on the colloidal characteristics of CS-TPP-NPs were investigated and the resulting nanoparticles were characterized using scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) and x-ray diffraction (XRD) analyses. Physicochemical properties, including particle size, zeta potential and polydispersity index (PDI) were examined, and in vitro release studies were conducted to ascertain the release profile of caffeine from the nanoparticles. In addition, the colloidal stability of the prepared NPs was also assessed on storage.

Results: Process parameters appeared to exert a significant effect on the physicochemical characteristics of the CS-TPP-NPs. The CS-TPP-NPs prepared under optimum conditions (CS concentration of 0.2 mg/ml, CS: TPP volume ratio of 25:12 ml, stirred at 700 rpm for 60 min, with 0.97 mg/ml caffeine concentration and treatment with low ultra-sonication for 30 min) had shown a mean particle size of ~143.43±1.69 nm, zeta potential of+43.13±1.10 mV, PDI of ~0.30±0.01. A drug loading capacity and encapsulation efficiency of 48.89% and 60.69%, respectively, were obtained. Cumulative release study for drug-loaded CS-NPs was significantly (p<0.001, paired t-test) higher (58.7% caffeine released) compared to control formulation (41.5% caffeine released) after 72 h. Stability studies conducted for 28 d showed that caffeine-loaded CS-NPs degraded much quicker when stored at 25 ⁰C than 4 ⁰C. It was also noted that caffeine-loaded CS-NPs in the freeze-dried form were unstable as the surface charge of nanoparticles dropped from positive zeta potential to-3.55 mV within 2 d at 4 ⁰C and at 25 ⁰C, surface charge dropped to-3.16 mV within 14 d of the experiment.

Conclusion: Chitosan (CS)–tripolyphosphate (TPP)–nanoparticles (NPs) appear to be a promising strategy to achieve sustained percutaneous delivery of caffeine.


Keywords


Chitosan nanoparticles, Drug delivery, Caffeine, Ionic gelation

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About this article

Title

SELF-ASSEMBLED CHITOSAN NANOPARTICLES FOR PERCUTANEOUS DELIVERY OF CAFFEINE: PREPARATION, CHARACTERIZATION AND IN VITRO RELEASE STUDIES

Keywords

Chitosan nanoparticles, Drug delivery, Caffeine, Ionic gelation

DOI

10.22159/ijap.2018v10i4.25947

Date

07-07-2018

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 10, Issue 4 (July-Aug), 2018 Page: 172-185

Online ISSN

0975-7058

Authors & Affiliations

Nik Amanina Farhanah Abu Hassan
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi Mara, Puncak Alam Campus 42300 Selangor, Malaysia
Malaysia

Shariza Sahudin
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi Mara, Puncak Alam Campus 42300 Selangor, Malaysia
Malaysia

Zahid Hussain
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi Mara, Puncak Alam Campus 42300 Selangor, Malaysia

Mumtaz Hussain
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi Mara, Puncak Alam Campus 42300 Selangor, Malaysia

Mumtaz Hussain
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi Mara, Puncak Alam Campus 42300 Selangor, Malaysia


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