Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

Abdulla, Juma Masoud Abdulla; Tan, Yvonne Tze-Fung; Darwis, Yusrida

doi:10.1208/s12249-010-9428-6

Cited by 28 publications

(20 citation statements)

References 33 publications

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“…50 Abdulla et al found that the release profile of rifampicin-SSMs followed both the firstorder and Higuchi kinetics models. 51 However, they only used the correlation coefficient to evaluate the goodness of fit. In our study, there were insignificant differences among the R 2 adjusted values following the first-order and Higuchi equation (P .…”

Section: Solubility and Budesonide Release From Ssmsmentioning

confidence: 99%

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Sahib¹,

Darwis²,

Peh³

et al. 2011

IJN

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Background: Inhaled corticosteroids provide unique systems for local treatment of asthma or chronic obstructive pulmonary disease. However, the use of poorly soluble drugs for nebulization has been inadequate, and many patients rely on large doses to achieve optimal control of their disease. Theoretically, nanotechnology with a sustained-release formulation may provide a favorable therapeutic index. The aim of this study was to determine the feasibility of using sterically stabilized phospholipid nanomicelles of budesonide for pulmonary delivery via nebulization. Methods: PEG 5000 -DSPE polymeric micelles containing budesonide (BUD-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and pharmacodynamic characteristics of BUD-SSMs were investigated. Results: The optimal concentration of solubilized budesonide at 5 mM PEG 5000 -DSPE was 605.71 ± 6.38 µg/mL, with a single-sized peak population determined by photon correlation spectroscopy and a particle size distribution of 21.51 ± 1.5 nm. The zeta potential of BUD-SSMs was −28.43 ± 1.98 mV. The percent entrapment efficiency, percent yield, and percent drug loading of the lyophilized formulations were 100.13% ± 1.09%, 97.98% ± 1.95%, and 2.01% ± 0.02%, respectively. Budesonide was found to be amorphous by differential scanning calorimetry, and had no chemical interaction with PEGylated polymer according to Fourier transform infrared spectroscopy. Transmission electron microscopic images of BUD-SSMs revealed spherical nanoparticles. BUD-SSMs exhibited prolonged dissolution behavior compared with Pulmicort Respules ® (P , 0.05). Aerodynamic characteristics indicated significantly higher deposition in the lungs compared with Pulmicort Respules ® . The mass median aerodynamic, geometric standard deviation, percent emitted dose, and the fine particle fraction were 2.83 ± 0.08 µm, 2.33 ± 0.04 µm, 59.13% ± 0.19%, and 52.31% ± 0.25%, respectively. Intratracheal administration of BUD-SSMs 23 hours before challenge (1 mg/kg) in an asthmatic/chronic obstructive pulmonary disease rat model led to a significant reduction in inflammatory cell counts (76.94 ± 5.11) in bronchoalveolar lavage fluid compared with administration of Pulmicort Respules ® (25.06 ± 6.91). Conclusion:The BUD-SSMs system might be advantageous for asthma or chronic obstructive pulmonary disease and other inflammatory airway diseases.

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Section: Solubility and Budesonide Release From Ssmsmentioning

confidence: 99%

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Sahib¹,

Darwis²,

Peh³

et al. 2011

IJN

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“…Moreover, a patient-friendly device that increases adherence and possibly enables monitoring of treatment should be investigated further 118. These parameters have been partially achieved with carriers (eg, liposomes, PEG, chitosan)53,58,63,69,71,72 encapsulating the antibiotic drug and with new aerosol production systems (eg, eFlow)124 and mouthpiece modifications 126. Three directions of investigation should summarized to (i) production system, (ii) efficient interface of production to deposition, and (iii) efficient local concentration (MIC max ) (Table 5).…”

Section: Resultsmentioning

confidence: 99%

Clinical experimentation with aerosol antibiotics: current and future methods of administration

Zarogoulidis¹,

Kioumis²,

Porpodis³

et al. 2013

DDDT

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Currently almost all antibiotics are administered by the intravenous route. Since several systems and situations require more efficient methods of administration, investigation and experimentation in drug design has produced local treatment modalities. Administration of antibiotics in aerosol form is one of the treatment methods of increasing interest. As the field of drug nanotechnology grows, new molecules have been produced and combined with aerosol production systems. In the current review, we discuss the efficiency of aerosol antibiotic studies along with aerosol production systems. The different parts of the aerosol antibiotic methodology are presented. Additionally, information regarding the drug molecules used is presented and future applications of this method are discussed.

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“…Abdulla et al. [] found that the release profile of rifampicin‐SSMs followed both the first‐order and Higuchi kinetics models. However, they only used the correlation coefficient to evaluate the goodness of fit.…”

Section: Resultsmentioning

confidence: 99%

Incorporation of Beclomethasone Dipropionate into Polyethylene Glycol‐Diacyl Lipid Micelles as a Pulmonary Delivery System

Sahib

Darwis

Peh

et al. 2012

Drug Development Research

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Strategy, Management and Health Policy Enabling Technology, Genomics, ProteomicsPreclinical ResearchPreclinical Development Toxicology, Formulation Drug Delivery, PharmacokineticsClinical Development Phases I‐III Regulatory, Quality, ManufacturingPostmarketing Phase IV Nebulized corticosteroid drugs have several shortcomings due to their poor water solubility and nonoptimal deposition pattern. The aims of this study were to investigate the in vitro and in vivo characteristics of beclomethasone dipropionate (BDP)‐loaded sterically stabilized phospholipid nanomicelles (SSMs) of a polyethylene glycol–phosphatidylethanolamine conjugate as a pulmonary delivery system. The particle size distribution and zeta potential measurements were 14.60 ± 1.11 nm and −46.94 ± 3.27 mV, respectively. The solubility of BDP was highly improved by at least 1,300 times its actual solubility. No chemical interaction was found between the PEGylated polymer and BDP as demonstrated by the Fourier transform infrared results. The in vitro aerodynamic of the aerosolized BDP‐SSMs using an Omron nebulizer showed an improvement in the aerodynamic values, with a significant deposition in the seven‐stage Next Generation Impactor. The BDP‐SSMs showed a prolonged dissolution profile of about 3 days. Intratracheal administration of the BDP‐SSMs (1 mg/kg) 12 or 23 h before a challenge in the asthmatic rat model led to a significant reduction in the inflammatory cell counts in bronchoalveolar lavage fluid samples compared with the administration of solubilized BDP. The SSM system appears to be an effective way of improving the therapeutic index of nebulized, poorly soluble corticosteroids.

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Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

Cited by 28 publications

References 33 publications

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Clinical experimentation with aerosol antibiotics: current and future methods of administration

Incorporation of Beclomethasone Dipropionate into Polyethylene Glycol‐Diacyl Lipid Micelles as a Pulmonary Delivery System

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