Arimoclomol-loaded Pluronic F127 nanomicelles in experimental endometriosis: drug incorporation, in vitro release, and early morphological and histological responses

Xavier-de-Britto I, Isabelle Xavier-de-Britto, Gomes-da-Silva NC, Natália Cristina Gomes-da-Silva, Natalia Cristina Gomes-da-Silva, Alencar LMR, Luciana Magalhães Rebelo Alencar, Luciana Magalhães Rebêlo Alencar, Rebelo Alencar LM, Ricci-Junior E, Eduardo Ricci-Junior, Pierre B A Fechine, Fechine PBA, Pierre Basílio Almeida Fechine, Cavalcanti ADS, Amanda Dos Santos Cavalcanti, Dos Santos Cavalcanti A, Alessandra Cristina Chagas Valim, Valim ACC, Chagas Valim AC, Jamila Alessandra Perini, Perini JA, Victor Branco de Sousa, de Sousa VB, Júnior SA, Severino Alves, Severino Alves Júnior, Daniel Escorsim Machado, Machado DE, Ralph Santos-Oliveira, Ralph Santos‐Oliveira, Santos-Oliveira R
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2026 · vol. 228 , pp. 115237 · doi:10.1016/j.ejpb.2026.115237 · PMID:42778111 · W7214111256
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Arimoclomol-loaded Pluronic F127 nanomicelles demonstrated 100% drug retention and biphasic release, inducing early morphological improvements in an experimental endometriosis rat model without short-term toxicity.

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Abstract

Endometriosis is a chronic, estrogen-dependent inflammatory disease characterized by ectopic endometrial-like glands and stroma, persistent pelvic inflammation, pain, infertility, and frequent recurrence. The limited availability of nonhormonal and lesion-directed therapies supports the investigation of alternative pharmacological mechanisms and regional drug-delivery strategies. Arimoclomol is a co-inducer of the endogenous heat-shock response with the capacity to amplify stress-dependent proteostasis, whereas Pluronic F127 is an amphiphilic PEO-PPO-PEO copolymer that forms drug-associated micellar assemblies in aqueous media. This exploratory study evaluated the physicochemical properties, in vitro release profile, and early biological response to arimoclomol-loaded Pluronic F127 nanomicelles in an autologous-transplantation rat model of endometriosis. The formulation was prepared by dispersing 30 mg of arimoclomol in 2 mL of Pluronic F127 at 20% (w/v), followed by stirring and ultrasonication under cooling. Because no centrifugation, filtration, dialysis, lyophilization, or other drug-removal step was applied after incorporation, the nominal process loading efficiency was 100%, based on formulation mass balance. The corresponding theoretical drug content was 6.98% w/w of total formulation solids and 7.5% w/w relative to the polymer mass. Drug-polymer association was supported by scanning electron microscopy coupled to energy-dispersive X-ray spectroscopy, Raman spectroscopy, and UV-Vis spectroscopy. In vitro dialysis at 37 °C showed a rapid increase in acceptor-medium arimoclomol concentration, reaching 14.33 ± 0.18 µg/mL at 2 h, followed by a progressive decline, with arimoclomol remaining detectable at 72 h (2.76 ± 0.04 µg/mL). Endometriosis was induced in ten female Wistar rats. On day 16, animals received a single intraperitoneal administration of arimoclomol-loaded nanomicelles (n = 4), empty nanomicelles (n = 3), or free arimoclomol (n = 3). The arimoclomol dose was 3 mg/animal, equivalent to approximately 14.7-16.8 mg/kg according to the recorded body-weight range. Twenty-four hours after treatment, representative lesions from the loaded-nanomicelle group appeared smaller macroscopically and showed mildly atrophic glands, stromal disorganization, and less prominent inflammatory infiltration than representative lesions from the empty-carrier and free-drug groups. All clinical welfare scores remained zero, and no overt short-term intolerance was observed. These findings demonstrate nominal quantitative drug retention based on process mass balance, a biphasic in vitro release pattern, and an early treatment-associated morphological and histological response. These preliminary findings require confirmation in larger, blinded, power-calculated studies with quantitative lesion endpoints, mechanistic biomarkers, lesion-specific pharmacokinetics, and longitudinal safety assessment.

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MeSH descriptors

Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Nanoparticles Nanoparticles Nanoparticles Nanoparticles Nanoparticles

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References (30)

SciLite annotations

chemicals 1
estrogen
organisms 4
zitter rats zitter rats multicellular animals rodents

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