RESUMEN
In situ gelling systems represent a burgeoning paradigm in ocular drug administration, addressing intrinsic challenges posed by extant ocular formulations, such as compromised bioavailability and constraints in traversing the corneal barrier. This systematic review endeavours to comprehensively examine the contemporary landscape of research in this domain, focusing on the nuanced capabilities of in situ gelling systems to optimize drug delivery and enhance therapeutic outcomes, without much technological complexity. Employing a meticulous search strategy across diverse databases for publications and patents spanning the years 2015 to 2023 a total of 26 research papers and 14 patents meeting stringent inclusion criteria were identified. Synthesizing the collective insights derived from these investigations, it becomes evident that in situ gelling systems confer an ability to protract the residence time of formulations or active pharmaceutical ingredients (APIs) within the ocular milieu. This sustained presence engenders extended drug release kinetics, thereby fostering improved patient compliance and mitigating the proclivity for side effects attendant to frequent dosing. These salutary effects extend to diminished systemic drug absorption, augmented ocular bioavailability, and the prospect of reduced dosing frequencies, thereby amplifying patient adherence to therapeutic regimens. Intriguingly, the protective attributes of in situ gelling systems extend to the establishment of an ocular surface barrier, thereby abating the susceptibility to infections and inflammatory responses. In summation, this review underscores the auspicious potential of in situ gelling systems as a transformative approach to advancing ocular drug delivery, warranting sustained research endeavours and developmental initiatives for the betterment of global patient outcomes.
Asunto(s)
Administración Oftálmica , Sistemas de Liberación de Medicamentos , Geles , Humanos , Animales , Disponibilidad Biológica , Ojo/metabolismo , Preparaciones Farmacéuticas/administración & dosificación , Preparaciones Farmacéuticas/química , Soluciones Oftálmicas/administración & dosificaciónRESUMEN
α, ß-Arteether (ART) antimalarial drug is used to treat chloroquine-resistant malaria and cerebral malaria. The drug's solubility in water is relatively low (17 µg/mL), and 40% of the drug degrades in the stomach, resulting in poor bioavailability. This article discusses the quality by design technique used for formulation development and optimization of nanostructured lipid carriers (NLCs). The ART-NLCs were made by solvent diffusion method. To develop solid NLCs, the NLCs were freeze-dried and encapsulated in enteric-coated capsule shells. The prepared NLCs showed particle size ranging between 156.8 ± 12 nm while zeta potential ranging between - 26.1 ± 0.22 mV. They also showed high encapsulation efficiency (> 85%) and an amorphous drug's lipid matrix state. Pharmacokinetic parameters of optimized formulation enhance oral bioavailability to 18.45%. These investigations demonstrated the superiority of NLCs for improvement of solubility as well as oral bioavailability of poorly water-soluble drugs.