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April 11, 2026Pharmaceutics2 citationsOpen Access

Innovative HPMC/PVP K90 Dissolving Microneedles Incorporating Tacrolimus-Loaded Cubosomes: A Novel Strategy for Managing Allergic Conjunctivitis

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SESammar Fathy ElhabalMSMai S. ShoelaFHFaraz Hassan

Key Points

  • Develop a non-invasive delivery system for tacrolimus to manage allergic conjunctivitis effectively.
  • Prepared tacrolimus-loaded cubosomes using a top-down fragmentation method.
  • Optimized formulation via Box–Behnken design and incorporated into dissolving microneedles.
  • Evaluated system in vitro, ex vivo, and in vivo using a rabbit model of allergic conjunctivitis.
  • Achieved smallest particle size of 210 nm with high entrapment efficiency (93.3%).
  • Demonstrated over 80% drug release over 24 hours, compared to 40% from suspension.
  • In vivo studies showed significant reductions in inflammatory markers by 50-75% and confirmed reduced inflammation without irritation.

Abstract

Background/Objectives: Allergic conjunctivitis (AC) is the most common inflammatory disease affecting the ocular conjunctiva. Tacrolimus (TCR), a potent calcineurin inhibitor, is limited by poor aqueous solubility and low ocular bioavailability. This study aimed to develop TCR-loaded cubosomes (TCR-Cubs) incorporated into HPMC/PVP K90 dissolving microneedles (MNs) to enhance their therapeutic efficacy. Methods: TCR-Cubs were prepared using a modified top-down fragmentation method with glyceryl monooleate and poloxamer 407, optimized via Box–Behnken design, and incorporated into dissolving MNs. The system was evaluated in vitro, ex vivo, and in vivo using a rabbit model of allergic conjunctivitis. Results: The optimized formulation exhibited the smallest particle size (210 ± 0.91 nm), polydispersity index (0.29 ± 0.03), zeta potential (−21 ± 0.87 mV), and the highest entrapment efficiency (% 93.3 ± 0.45). The optimized formulation was incorporated into MNs via micro molding. Scanning electron microscopy (SEM) confirmed well-defined, sharp microneedles, with low height reduction (85–90%). In vitro release studies revealed sustained drug release of (~75–80%) over 24 h, compared to (~40%) from the TCR suspension, following diffusion-controlled kinetics. Ex vivo permeation studies showed a (~2–3-fold) enhancement in corneal drug flux. In vivo pharmacodynamic evaluation using an ovalbumin-induced allergic conjunctivitis model demonstrated significant reductions in inflammatory mediators, including inflammatory markers (TNF-α, IL-1β, IL-6, NLRP3), which were reduced by (~50–75%), with modulation of CPA3, BCL2, and TGF-β1 by qRT-PCR. Histopathology and TLR4 analysis confirmed reduced inflammation without irritation. Conclusions: This dual-delivery system offers a promising, non-invasive platform for enhanced ocular delivery of tacrolimus with superior anti-inflammatory efficacy in allergic conjunctivitis.

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Cite This Study

Elhabal et al. (2026) studied this question.

synapsesocial.com/papers/69d9e5b378050d08c1b75ed7https://doi.org/10.3390/pharmaceutics18040459
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Dose-Sparing Topical Administration: FK506-Loaded Nano-Micelles Achieve Efficient Therapy in a Murine Model of Vernal Keratoconjunctivitis2026
  2. 2Enhanced Ocular Delivery of Tacrolimus via Cationic Nanoliposomes: Mitigating Inflammation and Rebalancing Th17/Treg Responses in Dry Eye Disease2026
  3. 3Injectable Thermoresponsive Dual Nanocarrier Hydrogel for Local Tacrolimus Delivery with a Two-Phase Release Profile2026
  4. 4Hyaluronic acid nanoparticle as drug delivery carrier for the treatment of allergic conjunctivitis2026
  5. 5Stimuli-Responsive Polymeric Conjugates of Tacrolimus: A pH/Redox-Triggered Approach toward Precision Drug Delivery2025