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Characterization of polymeric micelles for pulmonary delivery of beclomethasone dipropionate

Gaber NN, Darwis Y, Peh KK, Tan YT

J Nanosci Nanotechnol, 2006 10 20;6(9-10):3095-101.
PMID: 17048523

The potential of using poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG-DSPE) polymer to prepare BDP-loaded micelles with high entrapment efficiency and mass median aerodynamic diameter of less than 5 microm demonstrating sustained release properties was evaluated. The result showed that lyophilized BDP-loaded polymeric micelles with entrapment efficiency of more than 96% could be achieved. Entrapment efficiency was affected by both the drug to polymer molar ratio and the amount of drug used. Investigation using FTIR and DSC confirmed that there was no chemical or physical interaction and the drug was molecularly dispersed within the micelles. TEM images showed that the drug-loaded polymeric micelles were spherical in shape with multivesicular morphology. Further analysis by photon correlation spectroscopy indicated that the particle size of the BDP-loaded micelles was about 22 nm in size. In vitro drug release showed a promising sustained release profile over six days following the Higuchi model. The mass median aerodynamic diameter and fine particle fraction were suitable for pulmonary delivery. Moreover, the small amount of deposited drug in the induction port (throat deposition) suggested possible reduction in incidence of oropharyngeal candidiasis, a side effect normally associated with inhaled corticosteroids therapy. The high encapsulation efficiency, comparable inhalation properties, sustained release behavior together with biocompatibility nature of the polymer support the potential of BDP-loaded polymeric micelles as a versatile delivery system to be used in the treatment of asthma and chronic obstructive pulmonary disease.

Matched MeSH terms: Beclomethasone/administration & dosage*; Beclomethasone/pharmacokinetics; Beclomethasone/chemistry*
Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations

Sahib MN, Abdulameer SA, Darwis Y, Peh KK, Tan YT

Drug Des Devel Ther, 2012;6:29-42.
PMID: 22393583

The local treatment of lung disorders such as asthma and chronic obstructive pulmonary disease via pulmonary drug delivery offers many advantages over oral or intravenous routes of administration. This is because direct deposition of a drug at the diseased site increases local drug concentrations, which improves the pulmonary receptor occupancy and reduces the overall dose required, therefore reducing the side effects that result from high drug doses. From a clinical point of view, although jet nebulizers have been used for aerosol delivery of water-soluble compounds and micronized suspensions, their use with hydrophobic drugs has been inadequate.

Matched MeSH terms: Beclomethasone/administration & dosage*; Beclomethasone/chemistry
Fulltext Pre and post treatment mucociliary function in allergic rhinitis in three different treatment modalities

Lee LM, Gendeh BS

Med J Malaysia, 2003 Mar;58(1):17-20.
PMID: 14556322

Allergic rhinitis causes an impairment of the mucociliary function in the nose. It is hoped that treatment of perennial allergic rhinitis would be able to revert mucociliary function to normal. This study aims to compare pre and post treatment mucociliary transport time in 3 different treatment modalities. Ninety-two newly diagnosed patients with allergic rhinitis were randomised into 3 groups and started on different treatment regimes. At the end of 8 weeks, the group treated with only intranasal beclomethasone showed some, though not significant, improvement in the mucociliary function. There were no changes in the mucociliary function in the other two groups treated with beclomethasone and loratidine or loratidine alone.

Study site: ENT clinic in Pusat Perubatan Universiti Kebangsaan Malaysia (PPUKM)
UKM

Matched MeSH terms: Beclomethasone/administration & dosage; Beclomethasone/therapeutic use*
The Relationship Between Long-term Use of Intranasal Corticosteroid and Intraocular Pressure

Mohd Zain A, Md Noh UK, Hussein S, Che Hamzah J, Mohd Khialdin S, Md Din N

J Glaucoma, 2019 04;28(4):321-324.
PMID: 30585941 DOI: 10.1097/IJG.0000000000001164

PURPOSE: The purpose of this study was to investigate the association between long-term intranasal steroid use and intraocular pressure (IOP) elevation.
PATIENTS AND METHODS: In total, 100 eyes from 50 patients on long-term intranasal steroids (>2 y) for allergic rhinitis and 90 eyes from 45 controls were included in this study. Patients on other forms of steroids and risk factors for glaucoma were excluded. IOP was measured and nonmydriatic stereoscopic optic disc photos were taken for each eye. The vertical cup-to-disc ratio and the status of the optic disc were evaluated.
RESULTS: The mean IOP for intranasal steroids group was significantly higher (15.24±2.31 mm Hg) compared to the control group (13.91±1.86 mm Hg; P=0.000). However, there were no significant differences in the vertical cup-to-disc ratio and the status of glaucomatous optic disc changes between the groups.
CONCLUSIONS: Prolonged use of intranasal steroids cause statistical significant increase in IOP in patients with allergic rhinitis although no significant glaucomatous disc changes were seen. We suggest patients on long-term use of intranasal steroid have a yearly eye examination to be monitored for IOP elevation and those with additional risk factors for glaucoma is closely monitored for glaucoma.

Matched MeSH terms: Beclomethasone/adverse effects