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Updated: May 29, 2025

Formulation of Diblock Polymeric Nanoparticles through Nanoprecipitation Technique
Published on: September 20, 2011
Physicochemical characterization and nanochemical analysis of ciprofloxacin hydrophobic ion Pairs for enhanced
Jong-Ju Lee1, Minji Choi1, Yuim Jeon1
1College of Pharmacy & Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon, 21983, Republic of Korea.
Abstract:
This study investigates the physicochemical transformation of ciprofloxacin (CIP) through hydrophobic ion pairing with five counter ions-sodium oleate, sodium laurate, sodium caprate, disodium pamoate, and sodium deoxycholate-to enhance compatibility with hydrophobic Poly (lactic-co-glycolic acid) (PLGA) nanoparticles. Complexation efficiencies (CE) reached up to 92.26 %, with ciprofloxacin pamoate (CIP-PAM) achieving over 90 % CE at a 1:0.5 M ratio. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analyses showed reduced crystallinity across all complexes, with CIP-PAM exhibiting an amorphous form. Optical photothermal infrared spectroscopy (O-PTIR) confirmed uniform complexation within particles, while CIP-PAM displayed a broad peak and weak intensity in the 900-1300 cm-1 region, supporting its amorphous nature. Log P values demonstrated increased hydrophobicity for all complexes, with ciprofloxacin oleate (CIP-OLE) showing a 93-fold increase (p < 0.001). In vitro dissociation patterns varied: CIP-OLE maintained steady release in DW (49.7 %) and PBS (32.3 %) over 48 h, whereas CIP-PAM exhibited strong stability in DW (25.2 %) and a contrasting 68.1 % release in PBS, highlighting solvent-dependent dissociation behaviors. PLGA nanoparticles prepared via S/O/W achieved particle sizes under 200 nm, with CIP-PAM showing the highest encapsulation efficiency (63.02 % vs 17.21 % (CIP)). These findings underscore the importance of counter ion selection to optimize CIP compatibility with hydrophobic carriers, providing a basis for improved drug loading of hydrophilic antibiotics.
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