Nano-crystallization as a tool for the enhancement of beclomethasone dipropionate dermal deposition: Formulation, in vitro characterization and ex vivo study

Assem, M. A.; Khowessah, Omneya Mohammed; Ghorab, Dalia

doi:10.1016/j.jddst.2019.101318

Cited by 10 publications

(6 citation statements)

References 43 publications

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“…BDP is a practically insoluble drug; in pure water, the solubility of BDP is in the range 0.1–2.4 μg/mL (0.12 ± 0.04 μg/mL [ 26 ], 2.17 μg/mL [ 27 ], 2.38 μg/mL [ 28 ], 0.16 μg/mL [ 29 ]). The different solubilities of BDP might result from the different measurement methods, crystal forms, and particle sizes of the drug [ 30 ].…”

Section: Resultsmentioning

confidence: 99%

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Chuang

Lin

et al. 2022

Polymers

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In this study, the enhanced solubilization performance of a poorly soluble drug, beclomethasone dipropionate (BDP), was investigated using hydroxypropyl-β-cyclodextrin (HP-β-CD) and ethanol. The enhanced solubility of the drug was determined using the phase solubility method and correlated as a function of both HP-β-CD and ethanol concentrations. The effective progress of drug solubility originated from the formation of cyclodextrin and BDP inclusion complexes and increase in the lipophilicity of the medium, by aqueous ethanol, for hydrophobic BDP. BDP and HP-β-CD composite particles were produced using supercritical assisted atomization (SAA) with carbon dioxide as the spraying medium, 54.2% (w/w) aqueous ethanol as the solvent, and an optimal amount of the dispersion enhancer leucine. The effect of the mass ratio of HP-β-CD to BDP (Z) on the in vitro aerosolization and in vitro dissolution performance of BDP–HP-β-CD composite particles was evaluated. The aerosolization performance showed that the fine particles fraction (FPF) of the composite particles increased with increasing mass ratio. The water-soluble excipient (HP-β-CD) effectively enhance the dissolution rate of BDP from composite particles. This study suggests that BDP–HP-β-CD composite particles produced using SAA can be employed in immediate-release drug formulations for pulmonary delivery.

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Section: Resultsmentioning

confidence: 99%

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Chuang

Lin

et al. 2022

Polymers

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“…High pressure homogenization To enhance the cutaneous targeting and photostability of tretinoin, a poorly water-soluble and unstable compound used in commercial creams and gels for treating acne vulgaris, nanosuspensions were produced using a straightforward precipitation approach. 105,106 The permeation and deposition of drugs were studied through skin diffusion tests on newborn pigs, while UV light exposure was used to assess the photostability of tretinoin (TRA). Additionally, an oil-inwater (O/W) nanoemulsion was created and evaluated as a suitable comparator.…”

Section: In Vitro and In Vivomentioning

confidence: 99%

Nanosuspension-Based Drug Delivery Systems for Topical Applications

Aldeeb,

Wilar,

Suhandi

et al. 2024

IJN

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Nanosuspensions have garnered recent attention as a promising strategy for mitigating the bioavailability challenges of hydrophobic drugs, particularly those characterized by poor solubility in both aqueous and organic environments. Addressing solubility issues associated with poorly water-soluble drugs has largely resolved the need to enhance drug absorption and bioavailability. As mucosal formulations and topical administration progress in the future, nanosuspension drug delivery, straightforward formulation techniques, and versatile applications will continue to be subjects of interest. Nanosuspensions have undergone extensive scrutiny in preparation for topical applications, encompassing ocular, pulmonary, and dermal usage. Among the numerous methods aimed at improving cutaneous application, nanocrystals represent a relatively recent yet profoundly intriguing approach. Despite the increasing availability of various nanosuspension products, primarily designed for oral administration, only a limited number of studies have explored skin permeability and drug accumulation in the context of nanosuspensions. Nevertheless, the scant published research unequivocally underscores the potential of this approach for enhancing cutaneous bioavailability, particularly for active ingredients with low to medium solubility. Nanocrystals exhibit increased skin adhesiveness in addition to heightened saturation solubility and dissolution rate, thereby augmenting cutaneous distribution. The article provides a comprehensive overview of nanosuspensions for topical application. The methodology employed is robust, with a well-defined experimental design; however, the limited sample size raises concerns about the generalizability of the findings. While the results demonstrate promising outcomes in terms of enhanced drug delivery, the discussion falls short of addressing certain limitations. Additionally, the references largely focus on recent studies, but a more diverse inclusion of historical perspectives could offer a more holistic view of the subject.

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“…Beclomethasone dipropionate (BDP) was used as a topical medication for treating AD via the formulation of nanocrystals, serving as an anti-inflammatory agent; the corresponding results revealed that when BDP-loaded nanocrystals were compared with Beclozone ® cream (Teva Pharmaceutical Industries, Parsippany, NJ, USA) (0.25% BDP cream), the optimized formulation showed higher drug deposition through mouse skin, despite reduced flux and low systemic exposure of the drug [ 135 ].…”

Section: Emerging Therapies and Therapeuticsmentioning

confidence: 99%

Unraveling Atopic Dermatitis: Insights into Pathophysiology, Therapeutic Advances, and Future Perspectives

Pareek,

Kumari,

Pareek

et al. 2024

Cells

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Atopic dermatitis (AD) is an inflammatory skin condition that frequently develops before the onset of allergic rhinitis or asthma. More than 10% of children are affected by this serious skin condition, which is painful for the sufferers. Recent research has connected the environment, genetics, the skin barrier, drugs, psychological factors, and the immune system to the onset and severity of AD. The causes and consequences of AD and its cellular and molecular origins are reviewed in this paper. The exploration of interleukins and their influence on the immunological pathway in AD has been facilitated by using relevant biomarkers in clinical trials. This approach enables the identification of novel therapeutic modalities, fostering the potential for targeted translational research within the realm of personalized medicine. This review focuses on AD’s pathophysiology and the ever-changing therapeutic landscape. Beyond the plethora of biologic medications in various stages of approval or development, a range of non-biologic targeted therapies, specifically small molecules, have emerged. These include Janus kinase (JAK) inhibitors like Baricitinib, Upadacitinib, and Abrocitinib, thus expanding the spectrum of therapeutic options. This review also addresses the latest clinical efficacy data and elucidates the scientific rationale behind each targeted treatment for atopic dermatitis.

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Nano-crystallization as a tool for the enhancement of beclomethasone dipropionate dermal deposition: Formulation, in vitro characterization and ex vivo study

Cited by 10 publications

References 43 publications

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Nanosuspension-Based Drug Delivery Systems for Topical Applications

Unraveling Atopic Dermatitis: Insights into Pathophysiology, Therapeutic Advances, and Future Perspectives

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