Formulation strategy and use of excipients in pulmonary drug delivery

Pilcer, Gabrielle; Amighi, Karim

doi:10.1016/j.ijpharm.2010.03.017

Cited by 640 publications

(398 citation statements)

References 106 publications

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“…[75][76][77] The deposition of the particles occurs mainly at near airway bifurcations, where the velocity of airfl ow is high and where changes in the direction of bulk airfl ow occurs, generating inertial forces. Such inertial forces induce the impaction of large particles onto the airway surface.…”

Section: Sizementioning

confidence: 99%

Design Advances in Particulate Systems for Biomedical Applications

Lima

Álvarez-Lorenzo

Mano

2016

Adv Healthcare Materials

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Particulate systems have been widely used as containers of drugs or cells with the purpose of releasing them in a particularThe search for more effi cient therapeutic strategies and diagnosis tools is a continuous challenge. Advances in understanding the biological mechanisms behind diseases and tissues regeneration have widened the fi eld of applications of particulate systems. Particles are no more just protective systems for the encapsulated drugs, but they play an active role in the success of the therapy. Moreover, particles have been explored for innovative purposes as templates for cells growth and as diagnostic tools. Until few years ago the most relevant parameters in particles formulation were the chemistry and the size. Currently, it is known that other physical characteristics can remarkably affect the performance of particulate systems. Particles with non-conventional shapes exhibit advantages due to the increasing circulation time in blood stream, less clearance by the immune system and more effi cient cell internalization and traffi cking. Creation of compartments has been found useful to control drug release, to tune the transport of substances across biological barriers, to supply the target with more than one bioactive agent or even to act as theranostic systems. It is expected that such complex shaped and compartmentalized systems improve the therapeutic outcomes and also the patient's compliance, acting as advanced devices that serve for simultaneous diagnosis and treatment of the disease, combining agents of very different features, at the same time. In this review, we overview and analyse the most recent advances in particle shape and compartmentalization and applications of newly designed particulate systems in the biomedical fi eld.

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Section: Sizementioning

confidence: 99%

Design Advances in Particulate Systems for Biomedical Applications

Lima

Álvarez-Lorenzo

Mano

2016

Adv Healthcare Materials

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“…The aerosol droplets were aspirated by a constant suction pump at an airflow rate of 20 l/ minute, on the opposite side of the aerosol beam. All experiments were performed at room temperature (20)(21)(22)(23)(24)(25) C) and ambient relative humidity (40-60%).…”

Section: Determination Of Droplet Sizementioning

confidence: 99%

“…We also studied formulations with other nonionic polyoxyethylene surfactants: Polysorbate 80 (PS-80), which is commonly used in commercially inhalable or injectable products, and Brij 35 (B-35), which is used in various protein methods but not in drug formulations. 19,22,25 They also stabilized the antibody during nebulization, limiting the formation of medium-sized and large aggregates (data not shown). However, the concentration required to stabilize the antibody during nebulization depended on the surfactant molecule (0.01% [w/v] for PS-80 vs. 0.0001% [w/v] for B-35), but was not correlated with CMC (0.0017% and 0.011% in water, respectively).…”

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confidence: 91%

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Effect of formulation on the stability and aerosol performance of a nebulized antibody

Respaud

Marchand

Parent

et al. 2014

mAbs

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“…Optimization of flowability and dispersibility of formulations are critically important to develop desirable inhalation powders (Pilcer & Amighi, 2010). Presence of lactose monohydrate types and sieve fractions as carriers is a strategy to improve dispersion properties of inhalation particles (Kaialy, Alhalaweh, Velaga, & Nokhodchi, 2012;Patil, Mahadik, & Paradkar, 2015).…”

Section: Dpi Formulationsmentioning

confidence: 99%

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

Wang¹

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Cigarette smoking has become one of the leading causes of preventable deaths all over the world, causing a serious threat to human wellbeing and a tremendous economic burden to governments. The currently available treatment options for smoking cessation are not efficient. The pulmonary delivery of drugs by methods such as dry powder inhaler (DPI) has been recognized as one of the most efficient routes of drug delivery to the targeted area. The lung delivery of nicotine in this way would be expected to mimic the effects of tobacco smoking and could significantly reduce the negative health effects of smoking that result from nicotine addiction.The aim of this study is to develop nanoparticles with controlled physicochemical properties using biodegradable polymer of chitosan (CS) loaded with nicotine salt for pulmonary delivery as DPI formulations. The outcomes of this project are expected to be a safe and effective CS-based nicotine formulation for pulmonary delivery to treat nicotine dependence. This thesis specially addresses the research questions: (1) how to develop a feasible process to manufacture the nanoparticles suitable for pulmonary drug delivery using biodegradable polymer of CS containing nicotine salt; (2) how to develop an animal model for pulmonary drug delivery from DPI formulation using a nose-only inhalation device.The current therapeutic options for treatment of smoking addiction have been reviewed, and current advancements of technology in pulmonary drug delivery are summarised. Buccal administration of drugs exhibits a low oral bioavailability, and sublingual tablets and chewing gums can be swallowed before being absorbed.Although nasal spray of nicotine is a fast way to deliver nicotine into the bloodstream, Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery iii the rate of absorption is still not as rapid as cigarette smoking. Therefore, it is proposed that delivery of nicotine with sustained drug release profile direct into the deep lung is likely to more effectively mimic the rapid effects of cigarette smoking on a physiological level, which could eliminate patient craving and allow the tapering of nicotine level over time to improve patients' compliance.Water in oil (w/o) emulsion crosslinking method has been used to fabricate nicotine hydrogen tartrate (NHT)-loaded CS nanoparticles which separate as solid microaggregates. The physicochemical properties of particles are characterized by a series of techniques. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) shows that the prepared particles are spherical in morphology with rough surface after loading CS particles with NHT. Dynamic Light Scattering (DLS)by Zetasizer determined nanoparticle size ranging from 167.6 nm to 411 nm, while DLS by Mastersizer demonstrated that the microaggregates of these nanoparticles are in the respirable range (<5µm). The surface positive charge as measured by zeta potential tends to decrease with increase of mass ratios of NHT to CS, which is in contr...

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Formulation strategy and use of excipients in pulmonary drug delivery

Cited by 640 publications

References 106 publications

Design Advances in Particulate Systems for Biomedical Applications

Design Advances in Particulate Systems for Biomedical Applications

Effect of formulation on the stability and aerosol performance of a nebulized antibody

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

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