Abstract
Intranasal administration has assumed in the last years an increasing value as an alternative strategy for the systemic adsorption of drugs, as an alternative to oral and parenteral routes thanks to the high vascularized nasal mucosa. Nevertheless, different drug features may restrict its absorption through the nasal mucosa with an insufficient diffusion to the systemic circulation. Several technological strategies are under investigation to improve drug absorption during nasal formulation design and production. The use of bioadhesive polymers can be considered a valid approach to pursue the aforementioned goal. Based on this consideration, Eudragit® Retard RS100 and RL100 resins were selected as positively charged copolymers to prepare polymeric NPs with potential mucoadhesive properties suitable for intranasal application. NPs were produced by the Quasi-emulsion Solvent Evaporation (QESD) method and loaded with diclofenac acid (DIC) or its epolamine salt (DIEP). Preliminary investigations were performed to obtain the optimized blank formulation and drugs loaded NPs evaluating different parameters that can affect particles size and polydispersity. The optimized formulations unloaded and loaded with DIC and DIEP were further evaluated for their thermotropic behavior by differential scanning calorimetry. Mucoadhesive evaluation was assessed by measuring variation in zeta potential and by turbidimetric assay after incubation of particles with mucin in simulated nasal fluid (SNF) at 37 °C at different time points (0, 1 and 24 h) compared to the pure suspensions. Stability of DIC and DIEP loaded NPs was also evaluated in SNF to predict potential aggregation phenomena after nasal administration. Finally, in vivo experiments showed absence of toxicity on the nasal mucosa of mice.
Highlights
IntroductionThe intranasal (IN) administration of drugs often appears as a valid alternative to oral route, that can experience limitations such as poor absorption in the gastrointestinal tract and hepatic first-pass effect, or the impossibility to administer the drug to unconscious patients, like in many emergency situations [1]
The intranasal (IN) administration of drugs often appears as a valid alternative to oral route, that can experience limitations such as poor absorption in the gastrointestinal tract and hepatic first-pass effect, or the impossibility to administer the drug to unconscious patients, like in many emergency situations [1].Due to the relatively large surface of nasal mucosa and the high level of vascularization, a drug administered intranasally can be quickly absorbed and distributed in the systemic circulation, offering a valid tool for the therapy of keen conditions, such as seizure or acute pain [2]
In this study we evaluated new colloidal systems for the IN delivery of DIC and Diclofenac epolamine (DIEP)
Summary
The intranasal (IN) administration of drugs often appears as a valid alternative to oral route, that can experience limitations such as poor absorption in the gastrointestinal tract and hepatic first-pass effect, or the impossibility to administer the drug to unconscious patients, like in many emergency situations [1]. Due to the relatively large surface of nasal mucosa and the high level of vascularization, a drug administered intranasally can be quickly absorbed and distributed in the systemic circulation, offering a valid tool for the therapy of keen conditions, such as seizure or acute pain [2]. Micro- and nanosized drug delivery systems (DDS) can modulate the rate or time of drug release in the nasal mucosa, definitely controlling drug local effect or its levels in the systemic circulation [6]
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