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August 16, 2026Drug DeliveryOpen Access

Preparation of a new fixed-combination carteolol-netarsudil ophthalmic solution via one-pot pH-adjusting solubilization strategy for glaucoma treatment

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Authors

DJDian JiaoTWTao WangTLTu Lu

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Overview

Preclinical formulation study demonstrates potent intraocular pressure reduction and neuroprotection in glaucoma models, suggesting a viable once-daily, preservative-free eye drop.

Key Points

  • To formulate a preservative-free, once-daily fixed-combination ophthalmic solution of carteolol hydrochloride and netarsudil dimesylate using a one-pot pH-adjusting solubilization strategy to improve glaucoma management.
  • Formulated a fixed combination of carteolol hydrochloride and netarsudil dimesylate using hydroxypropyl methylcellulose (HPMC) as a thickener at pH ~5.0 (FC-CN-TKN).
  • Assessed physicochemical stability under refrigerated conditions along with pharmacokinetic intraocular penetration and precorneal retention.
  • Evaluated intraocular pressure (IOP) reduction and retinal ganglion cell neuroprotection following once-daily administration.
  • The one-pot pH-adjusting formulation resolved drug precipitation issues, maintaining high physicochemical stability under refrigeration without hindering intraocular penetration.
  • Addition of HPMC prolonged precorneal residence time, leading to improved ocular bioavailability.
  • Once-daily dosing of FC-CN-TKN demonstrated potent intraocular pressure-lowering efficacy and provided neuroprotective effects for retinal ganglion cells.

Cite This Study

Jiao et al. (2026) studied this question.

synapsesocial.com/papers/6a817a91f2fb91fc834ae705https://doi.org/10.1080/10717544.2026.2708376
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