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<p>The current study aimed at development of acetazolamide loaded pectin-chitosan nanocapsules (APCNC) via a polyelectrolyte complex coacervation technique, further incorporated into a poloxamer 407 and HPMC-based in situ gel (APCNC-ISG). The resulting APCNC demonstrated a positive zeta potential (+ 23.45 ± 0.30 mV), high entrapment efficiency (94.33 ± 1.2%), small hydrodynamic size (104 ± 2.4&#xa0;nm), and narrow size distribution (PDI &lt; 0.3). The SEM and TEM analyses confirmed the spherical morphology and nano range size of APCNC, while XRD analysis revealed the conversion of acetazolamide from a crystalline to an amorphous state. The APCNC-ISG exhibited pseudoplastic rheology with a gelling temperature of 36 ± 0.5&#xa0;°C and rapid gelation within 10 ± 2&#xa0;s. Furthermore, texture analysis displayed suitable adhesive properties. In vitro drug release and ex vivo permeation studies showed a sustained drug release over an extended period. The HET-CAM test and histopathological evaluation confirmed the non-irritating and non-toxic nature of the formulation, supporting its suitability for ophthalmic use. Pharmacodynamic studies demonstrated that APCNC-ISG significantly reduced intraocular pressure and maintained the effect for a prolonged duration compared to other formulations. These findings suggest that APCNC-ISG is a promising, adaptable, and effective drug delivery system for the treatment of glaucoma.</p> Graphical abstract <p></p>

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Thermosensitive in situ gel powered by pectin-chitosan nanocapsules for intraocular delivery of acetazolamide: in vitro, ex vivo, and in vivo evaluation

  • 期刊论文

  • 发表日期：

    2025年10月24日

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  • Uddhav Bagul,
  • Shubham Khot,
  • Ashish Monde,
  • Kiran Ashtekar,
  • Sivakumar Moni,
  • Chandrakant Kokare,
  • Amol Tagalpallewar

摘要

The current study aimed at development of acetazolamide loaded pectin-chitosan nanocapsules (APCNC) via a polyelectrolyte complex coacervation technique, further incorporated into a poloxamer 407 and HPMC-based in situ gel (APCNC-ISG). The resulting APCNC demonstrated a positive zeta potential (+ 23.45 ± 0.30 mV), high entrapment efficiency (94.33 ± 1.2%), small hydrodynamic size (104 ± 2.4 nm), and narrow size distribution (PDI < 0.3). The SEM and TEM analyses confirmed the spherical morphology and nano range size of APCNC, while XRD analysis revealed the conversion of acetazolamide from a crystalline to an amorphous state. The APCNC-ISG exhibited pseudoplastic rheology with a gelling temperature of 36 ± 0.5 °C and rapid gelation within 10 ± 2 s. Furthermore, texture analysis displayed suitable adhesive properties. In vitro drug release and ex vivo permeation studies showed a sustained drug release over an extended period. The HET-CAM test and histopathological evaluation confirmed the non-irritating and non-toxic nature of the formulation, supporting its suitability for ophthalmic use. Pharmacodynamic studies demonstrated that APCNC-ISG significantly reduced intraocular pressure and maintained the effect for a prolonged duration compared to other formulations. These findings suggest that APCNC-ISG is a promising, adaptable, and effective drug delivery system for the treatment of glaucoma.

Graphical abstract