ABSTRACT
Nasal drug delivery efficiency is highly dependent on the position in which the drug is deposited in the nasal cavity. However, no reliable method is currently available to assess its impact on delivery performance. In this study, a biomimetic nasal model based on three-dimensional (3D) reconstruction and three-dimensional printing (3DP) technology was developed for visualizing the deposition of drug powders in the nasal cavity. The results showed significant differences in cavity area and volume and powder distribution in the anterior part of the biomimetic nasal model of Chinese males and females. The nasal cavity model was modified with dimethicone and validated to be suitable for the deposition test. The experimental device produced the most satisfactory results with five spray times. Furthermore, particle sizes and spray angles were found to significantly affect the experimental device's performance and alter drug distribution, respectively. Additionally, mometasone furoate (MF) nasal spray (NS) distribution patterns were investigated in a goat nasal cavity model and three male goat noses, confirming the in vitro and in vivo correlation. In conclusion, the developed human nasal structure biomimetic device has the potential to be a valuable tool for assessing nasal drug delivery system deposition and distribution.
ABSTRACT
Intranasal drug delivery system is a non-invasive drug delivery route with the advantages of no first-pass effect, rapid effect and brain targeting. It is a feasible alternative to drug delivery via injection, and a potential drug delivery route for the central nervous system. However, the nasal physiological environment is complex, and the nasal delivery system requires "integration of medicine and device". Its delivery efficiency is affected by many factors such as the features and formulations of drug, delivery devices and nasal cavity physiology. Some strategies have been designed to improve the solubility, stability, membrane permeability and nasal retention time of drugs. These include the use of prodrugs, adding enzyme inhibitors and absorption enhancers to preparations, and new drug carriers, which can eventually improve the efficiency of intranasal drug delivery. This article reviews recent publications and describes the above mentioned aspects and design strategies for nasal intranasal drug delivery systems to provide insights for the development of intranasal drug delivery systems.
Subject(s)
Administration, Intranasal , Drug Delivery Systems , Pharmaceutical Preparations , Drug Carriers , Brain , Nasal Cavity/physiology , Nasal MucosaABSTRACT
Objective To prepare an in situ gel system for nasal delivery of menthol and to evaluate the safety of this formulation.Methods Menthol in situ gel was prepared with deacetylatedgellan gum.The nasal mucocilia toxicities of this formulation was evaluated using in situ toad palate model.Guinea pig skin sensitization test and the rabbit skin irritation test were conducted.Skin allergy and irritation reaction were monitored and scored.Results No significant effect on nasal mucosa ciliary movement and the morphology of rat nasal mucosa were observed.The formulation did not induce any dermal irritation in rabbits.Skin allergic reaction was not found in guinea pigs.Conclusion The preparation of menthol in situ nasal gel with low ciliary toxicity was easily achieved.This gel has good physiological flexibility.The further investigation was warranted for this formulation as an intranasal drug delivery system.
ABSTRACT
Incidence of neurodegenerative diseases has been increasing year by year in the current aging society which inter?feres the living quality of the patients severely. Pathological changes in neurodegenerative diseases appeare in central nervous system (CNS). The administration route of drugs to treat neurodegenerative diseases becomes a very important scientific research field. Part of drugs may cross over blood-brain barrier(BBB)to CNS by oral or injection administration. But most of drugs are distributed in the oth?er tissues and might cause adverse reactions ,such as gastrointestinal side-effects and arrhythmia. Moreover ,the compliance of the aging patients is poor. They cannot adhere to administer multi-dose drugs for sereral times a day. Nasal drug delivery systems could de?liver drugs to brains directly by nasal-brain route,avoiding BBB with high targeting ratio,high drug availability and good patients′compliance. The review summarizes the major types of neurodegenerative diseases and their current therapeutic methods. The impor?tant obstacles for brain-targeted drug delivery ,nose-brain routes and the factors influencing nasal absorption are introduced. More importantly,the principal formulations,recent research progress and the unsolved problems of brain-targeted nasal drug delivery sys?tems are also reviewed.
ABSTRACT
Incidence of neurodegenerative diseases has been increasing year by year in the current aging society which interferes the living quality of the patients severely. Pathological changes in neurodegenerative diseases appeare in central nervous system CNS . The administration route of drugs to treat neurodegenerative diseases becomes a very important scientific research field. Part of drugs may cross over blood-brain barrier BBB to CNS by oral or injection administration. But most of drugs are distributed in the other tissues and might cause adverse reactions, such as gastrointestinal side-effects and arrhythmia. Moreover, the compliance of the aging patients is poor. They cannot adhere to administer multi-dose drugs for sereral times a day. Nasal drug delivery systems could deliver drugs to brains directly by nasal-brain route, avoiding BBB with high targeting ratio, high drug availability and good patients’ compliance. The review summarizes the major types of neurodegenerative diseases and their current therapeutic methods. The important obstacles for brain-targeted drug delivery, nose-brain routes and the factors influencing nasal absorption are introduced. More importantly, the principal formulations, recent research progress and the unsolved problems of brain-targeted nasal drug delivery systems are also reviewed.
ABSTRACT
Nasal drug delivery systems prepared from natural materials are gaining importance in the field of pharmaceutical technology. Mucilage isolated from Linum usitatissimum L. (LUM) seeds was reported to be an effective natural mucoadhesive agent. The present study deals with a comparison of various characteristics of nasal gels containing midazolam hydrochloride (HCl) prepared from mucoadhesive agent extracted from Linum usitatissimum L. seeds and synthetic polymers like HPMC and Carbopol 934P in terms of texture profile analysis, mucoadhesive strength, and in vivo drug absorption profiles. It was observed that gels formulated with the natural mucilage showed better results than the synthetic gels in all aspects like hardness, adhesiveness, cohesiveness and mucoadhesive strength. The absolute bioavailability of midazolam hydrochloride from the natural gel was 97.55 percent whereas that of synthetic gels was 57.33 percent and 76.81 percent respectively.
Sistemas de liberação nasal preparados com produtos naturais estão ganhando importância no campo da tecnologia farmacêutica. A mucilagem isolada de sementes de Linum usitatissimum L. (LUM) mostrou-se agente mucoadesivo eficaz. O presente estudo trata da comparação de várias características de géis nasais contendo cloridrato de midazolam preparados com agente mucoadesivo extraído das sementes de Linum usitatissimum L. e com polímeros sintéticos, como HPMC e Carbopol 943P, com relação ao perfil de textura, força mucoadesiva e perfis de absorção do fármaco in vivo. Observou-se que os géis formulados com mucilagem natural apresentam melhores resultados do que os sintéticos em todos os aspectos, como dureza, adesão, coesão e força mucoadesiva. A biodisponibilidade absoluta do cloridrato de midazolam a partir do gel natural foi de 97,55 por cento, enquanto que nos géis sintéticos foi de 57,33 por cento e 76,81 por cento, respectivamente.
Subject(s)
Nasal Decongestants/pharmacokinetics , /therapeutic use , Plant Mucilage/pharmacokinetics , Midazolam/pharmacokinetics , AdhesivenessABSTRACT
The nasal route is one of the most permeable and highly vascularized site for ensuring rapid drug absorption and onset of therapeutic action. It has been potentially explored as an alternative route for delivery of drugs with poor bioavailability and for the biosensitive and high molecular weight compounds such as proteins, peptides, steroids, vaccines,etc. In this review nasal drug delivery approach and its limitations, some factors influencing drug absorption,mucoadhesion, and the safety of nasal mucoadhesive drug delivery systems as well were discussed.