Inhalable nanocomposite microparticles: preparation, characterization and factors affecting formulation

Elsayed, Ibrahim; AbouGhaly, Mohamed H.H.

doi:10.1517/17425247.2016.1102224

Cited by 23 publications

(16 citation statements)

References 117 publications

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“…Patients with respiratory disorders are usually administered their medications via inhalation 1. Pulmonary drug delivery offers several merits including its ability to attend higher drug levels at the site of its action, the lung, without the induction of systemic side effects 2.…”

Section: Introductionmentioning

confidence: 99%

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<p>Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery</p>

Mehanna

Mohyeldin

Elgindy

2019

IJN

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PurposeRifampicin, a first-line anti-tuberculosis drug, was loaded into a carbohydrate-based spray-dried nanocomposite with the aim to design a dry powder inhalation formulation. This strategy can enable efficient distribution of rifampicin within the lungs, localizing its action, enhancing its bioavailability and reducing its systemic exposure consequently side effects.MethodsThe respirable nanocomposite was developed utilizing spray drying of rifampicin nanosuspension employing a combination of mannitol, maltodextrin and leucine as microparticles matrix formers. Detailed physicochemical characterization and in-vitro inhalation properties of the nanocomposite particles were investigated. Compatibility studies were carried out using differential scanning calorimetry and Infrared spectroscopy techniques. Moreover, pulmonary in-vitro cytotoxicity on alveolar basal epithelial cells was performed and evaluated.ResultsNanocomposite-based rifampicin-loaded dry inhalable powder containing maltodextrin, mannitol and leucine at a ratio of 2:1:1 was successfully formulated. Rifampicin loading efficiency into the carbohydrate nanocomposite was in the range of 89.3% to 99.2% w/w with a suitable particle size (3.47–6.80 µm) and unimodal size distribution. Inhalation efficiency of the spray-dried nanosuspension was significantly improved after transforming into an inhalable carbohydrate composite. Specifically, mannitol-based powder had higher respirable fraction (49.91%) relative to the corresponding formulation of maltodextrin. Additionally, IC50 value of rifampicin nanocomposite was statistically significantly higher than that of free drug thus providing superior safety profile on lung tissues.ConclusionThe obtained results suggested that spray drying of rifampicin nanosuspension utilizing carbohydrates as matrix formers can enhance drug inhalation performance and reduce cellular toxicity. Thus, representing an effective safer pulmonary delivery of anti-tuberculosis drugs.

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Section: Introductionmentioning

confidence: 99%

“…In addition, local direct delivery of the drug into the airways is capable of creating fast onset of action with high therapeutic ratio 3. However, the airway geometry of the lungs poses a challenge for delivery into the alveoli 1…”

Section: Introductionmentioning

confidence: 99%

<p>Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery</p>

Mehanna

Mohyeldin

Elgindy

2019

IJN

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“…Pulmonary delivery via inhalation is a common technique of drug administration to patients with a variety of lung diseases. But the airway geometry of the lungs poses a challenge for delivery into the alveoli [14,15] . However, delivery of individual nanoparticles to the lungs appears to be a problematic, as due to their small sizes (< 1μm) which increased their probability of exhalation before deposition [16] .…”

Section: Targeted Inhalable Nanoparticle For Lung Carcinomamentioning

confidence: 99%

“…The differences between microparticles and nanoparticles extend beyond just the size, having larger surface area to volume ratios. Nanoparticles can have a higher drug loading capacity, using less polymers, better cross permeability barriers, increased cellular uptake, longer lung retention and in airway nanoparticles have better chances of mucus penetration [14] . This improves dissolution properties where decreasing the particle size increases the solubility and intracellular drug delivery potential.…”

Section: Dry Powder Inhalers and Nanoparticulate Powders For Inhalationmentioning

confidence: 99%

Inhalable nano-embedded microspheres as an emerging way for local treatment of lung carcinoma: Benefits, Methods of preparation & characterizaton

Gaber¹,

Nafee²,

Abdallah³

2021

Ad Med Pharma Den RE

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Lung cancer is the leading cause of cancer deaths worldwide, and this makes it an attractive disease to review and possibly improve therapeutic treatment options. The extreme lethality of lung cancer is ascribed to the lack of early diagnostic strategies as in almost 50 % of the cases the disease is confirmed in stage IV, leaving low chance of survival. The inaccessibility to the deeper portions of the lung for conventional therapy further adds up to the complication in the treatment process. Surgery, radiation, chemotherapy, targeted treatments, and immunotherapy separate or in combination are commonly used to treat lung cancer. However, these treatment types may cause different side effects, and chemotherapy-based regimens appear to have reached a therapeutic plateau. Hence, effective, better-tolerated treatments are needed to address and hopefully overcome this conundrum. Nanocarriers through inhalational route offer many advantages like; 1) they achieve uniform distribution of drug among the alveoli, 2) better solubilization of the drug, 3) sustained drug release which subsequently decreases dosing frequency, 4) better patient compliance, 5) lesser side effects, and 6) improved drug internalization to the cells. Therefore, targeted inhalable NP delivery to the lungs is a potential area of research in cancer nanotechnology that catches the attention of many formulation scientists, oncologists, and biomedical researchers. Based on this literature review, we will discuss the development, characterization, and benefits of inhalable nanocarriers for local treatment of lung carcinoma.

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“…Hygroscopicity and moisture retention are two important factors in hydrogel for clinical medicine application. [33][34][35] Previous study revealed that the Cu-MOP hydrogel was formed based on forming hydrogen bonds between Cu-MOPs and water molecules. Unfortunately, the ability of Cu-MOP hydrogel to maintain moist microenvironment was only for a very short time.…”

Section: Hygroscopicity and Moisture Retention Of The Paa-cu-mop Hydrogelmentioning

confidence: 99%

A biocompatible PAA-Cu-MOP hydrogel for wound healing

Chen

Qin

Cheng³

et al. 2020

RSC Adv.

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Inhalable nanocomposite microparticles: preparation, characterization and factors affecting formulation

Abstract: Nanocomposite microparticles have been found to be superior to both nanoparticles and microparticles and may represent a promising carrier for pulmonary drug delivery.

Cited by 23 publications

References 117 publications

<p>Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery</p>

<p>Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery</p>

Inhalable nano-embedded microspheres as an emerging way for local treatment of lung carcinoma: Benefits, Methods of preparation & characterizaton

A biocompatible PAA-Cu-MOP hydrogel for wound healing

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