Design of Intranasal Dosage Forms: Biopharmaceutical Aspects

Демина, Н. Б.; Бахрушина, Е. О.; Bardakov, A.I.; Краснюк, Иван Иванович

doi:10.29296/25419218-2019-03-02

Cited by 4 publications

(6 citation statements)

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“…Рост исследовательского интереса к разработке интраназальных in situ систем связан с их преимуществами, неоднократно отмечаемыми в различных работах. Реверсивные системы обеспечивают устойчивое и пролонгированное действие препарата, улучшенную комплаентность пациента и снижение частоты введения препарата по сравнению с обычной системой доставки лекарственных средств [1,3,5,6].…”

Section: ретроспектива систем доставки In Situunclassified

“…В зависимости от рода стимула, потенцирующего фазовый переход, матрицы in situ систем можно разделить на термореверсивные, рН-зависимые, ионночувствительные, влагоактивизируемые и др. [1].…”

Section: скрининг полимеров для In Situ гелеобразованияunclassified

“…Для коррекции и улучшения свойств готовых фармацевтических композиций зачастую используют не монокомпонентные матрицы, а смеси полимеров, обладающих идентичными или же различными механизмами in situ, гелеобразования [12]. Широко известна технология получения поликомплексов на основе полоксамера 407, когда для улучшения свойств биоадгезии в матрицу геля полоксамера добавляют мукоадгезивные полимеры с молекулярным весом выше 100 кДа, такие как редкосшитые акриловые полимеры карбополы, хитозан, а также различные производные целлюлозы: натрий-карбоксиметилцеллюлозу, гидроксипропилметилцеллюлозу, гидроксипропилцеллюлозу и метилцеллюлозу [1].…”

Section: скрининг полимеров для In Situ гелеобразованияunclassified

“…Интраназальный способ введения -один из самых перспективных неинвазивных способов доставки лекарственных веществ в организм человека. Этот путь введения обеспечивает высокую приверженность пациентов терапии, поскольку не требует привлечения медицинского персонала, не травматичен, легко осуществляем и высокоэффективен [1]. Возможность интраназального введения препаратов для обеспечения экстренной помощи используется на протяжении десятилетий медицинскими службами и службами безопасности многих стран при передозировке наркотиками, экстренной остановке сердцакак альтернатива внутривенным инъекциям [2].…”

Section: Introductionunclassified

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<i>In situ</i> Intranasal Delivery Systems: Application Prospects and Main Pharmaceutical Aspects of Development (Review)

Бахрушина

Демина

Shumkova

et al. 2021

Razrabotka i registraciâ lekarstvennyh sredstv

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Introduction. Intranasal delivery of in situ gel-forming systems is a complex but promising direction. Due to the high cost of developing a new chemical object or genetically engineered modification of biological molecules, pharmaceutical companies are focusing on developing technologies for new delivery systems for existing active pharmaceutical ingredients to improve their effectiveness and bioavailability. In situ systems for intranasal delivery, due to increased viscosity and mucoadhesion to the nasal mucosa, allow overcoming mucociliary clearance and ensuring complete absorption and prolonged release of drugs.Text. The article discusses the main advantages of intranasal in situ delivery systems shown in preclinical studies, as well as approaches to the technology of obtaining and standardization of these systems. The results of scientific research in this field over the past 15 years are summarized, the most promising polymers for creating thermoreversible and pH-sensitive compositions are identified, and modern methods for evaluating the sol-gel transition in situ are analyzed.Conclusion. The use of in situ systems for intranasal administration allows providing a high targeting of the delivery of synthetic and biological molecules to the brain. Currently, numerous pharmacokinetic and pharmacodynamic preclinical studies confirm the effectiveness of such systems, as well as their safety. Thermoreversible commercially available and directionally synthesized polymers (poloxamer 407, PLGA, NIPAAm, etc.), as well as chitosan, remain the most popular for the design of in situ delivery systems. In vitro and ex vivo methods with mucosa and artificial nasal fluid are widely used to assess the parameters of in situ gelation, but to increase the reproducibility of the methods and improve the correlation in vitro/in vivo, it is recommended to conduct modeling of the nasal cavity. Developing the technology and methods of screening of intranasal reversible systems will help to get closer to clinical trials and the entry of these delivery systems into the global pharmaceutical market.

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Section: ретроспектива систем доставки In Situunclassified

Section: скрининг полимеров для In Situ гелеобразованияunclassified

Section: Introductionunclassified

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<i>In situ</i> Intranasal Delivery Systems: Application Prospects and Main Pharmaceutical Aspects of Development (Review)

Бахрушина

Демина

Shumkova

et al. 2021

Razrabotka i registraciâ lekarstvennyh sredstv

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“…Nasal fluid has a pH of approximately 6.0 and an approximate ionic composition that can be reproduced in vitro using a solution of NaCl, KCl, and CaCl 2 (15:5:1) [ 4 ].…”

Section: Introductionmentioning

confidence: 99%

Intranasal Ion-Triggered In Situ Delivery System of Virus-like Particles: Development Using the Quality by Design Approach

Bakhrushina,

Mikhel,

Kondratieva

et al. 2024

Polymers

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The rapid growth in the prevalence of infectious diseases requires timely action from drug developers. In recent years, the COVID-19 pandemic has demonstrated the unpreparedness of the population for such emergencies. The introduction of modern methods of Design of Experiments (DoE) is required to accelerate the process of drug development and bring a drug to market. The main objective of this study was to develop an ion-triggered in situ system for intranasal delivery of VLP using a Quality by Design approach. Based on a literature review and initial studies, the key QTPP, CQA, CPP, and CMA were identified to develop a novel delivery system for virus-like particles. As a result of the studies on the quality attributes of the developed delivery system, an ion-triggered in situ gel meeting all the specified parameters was obtained using the Quality by Design method.

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Application of in Vitro Modeling for Pharmaceutical Development of in Situ Systems

E.O.

2022

Mediko-farmacevtičeskij žurnal "Pulʹs"

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Abstract. In vitro modeling of organs, tissues and systems is used to evaluate biopharmaceutical parameters of dosage forms and delivery systems – a trend that has been developing since the second half of the 20th century. One of the first among such models were devices for determining the parameter "Dissolution" of solid dosage forms. Today, with the growing research interest in the creation of new delivery systems, including stimulus–sensitive systems in situ, the scientific community needs a larger range of in vitro models that provide not only physiological counting actual parameters - pH of the biological fluid medium, temperature, clearance rate, which are taken into account in most modern models, but also special, potentiating the phase transition for in situ systems – the exact reproduced ionic composition of the liquid and mucose, the nature of the soft tissues on which the application is performed, etc. Such parameters can be used both in ready-made validated devices, by setting modified techniques, and when creating fundamentally new in vitro models. For example, in 2021, on the basis of the Department of Pharmaceutical Technology of the Institute of Pharmacy named after A.P. Nelyubin of Sechenov University, a model of the nasal cavity made of sculptural plasticine was developed and validated in vitro. The developed model was irrigated with a solution reproducing the mineral composition of nasal fluid before each experiment. The irrigation solution of the model contained 4% (m/V) mucin of pig stomach type II (Sigma Aldrich), which is a mixture of glycoproteins secreted by pig digestive glands with a content of N-acetyl-neuramic acid – 0.5%. For the in vitro experiment, the model was placed in a thermostat and kept at a temperature of 37℃ for 5-10 minutes. The developed nasal cavity model is successfully used for screening of intranasal pharmaceutical compositions both in the form of classical sprays, mucoadhesive systems, and stimulus-sensitive (thermo-, pH- or ion-selective) in situ systems.

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Design of Intranasal Dosage Forms: Biopharmaceutical Aspects

Cited by 4 publications

References 0 publications

<i>In situ</i> Intranasal Delivery Systems: Application Prospects and Main Pharmaceutical Aspects of Development (Review)

<i>In situ</i> Intranasal Delivery Systems: Application Prospects and Main Pharmaceutical Aspects of Development (Review)

Intranasal Ion-Triggered In Situ Delivery System of Virus-like Particles: Development Using the Quality by Design Approach

Application of in Vitro Modeling for Pharmaceutical Development of in Situ Systems

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