Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug

Hirun, Namon; Kraisit, Pakorn

doi:10.3390/polym14163406

Cited by 14 publications

(8 citation statements)

References 49 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…LEU exhibited a sharp endothermic peak at 307.5 °C related to the melting point, reflecting its highly crystalline structure [ 54 ]. HPMC exhibited a broad endothermic peak at 82.1 °C related to the water loss event, with no melting peak when heating up to 320 °C, reflecting its amorphous nature [ 55 ]. CsA-LEU, composed of LEU and CsA, exhibited a broad endothermic peak from LEU, and the endothermic peaks of CsA were not observed.…”

Section: Resultsmentioning

confidence: 99%

Development of Large Hollow Particles for Pulmonary Delivery of Cyclosporine A

Huang,

Tang,

Meng

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

The purpose of this study was to prepare large hollow particles (LHPs) by spray drying for pulmonary delivery of cyclosporine A (CsA), using L-Leucine (LEU) and hydroxypropyl methylcellulose (HPMC) as excipients and ammonium bicarbonate (AB) as a porogen. The prepared LHPs were spherical particles composed of both CsA and LEU on the surface and HPMC on the inner layer. The formulation of CsA-LEU-0.8HPMC-AB as typical LHPs showed excellent in vitro aerodynamic performance with a minimum mass median aerodynamic diameter (MMAD) of 1.15 μm. The solubility of CsA-LEU-0.8HPMC-AB was about 5.5-fold higher than that of raw CsA, and the dissolution of CsA-LEU-0.8HPMC-AB suggested that the drug was released within 1 h. The cell viability of the A549 cell line showed that CsA-LEU-0.8HPMC-AB was safe for delivering CsA to the lungs. In addition, inhalation administration of CsA-LEU-0.8HPMC-AB with the Cmax and AUC0–∞ increasing by about 2-fold and 2.8-fold compared with the oral administration of Neoral® could achieve therapeutic drug concentrations with lower systemic exposure and significantly improve the in vivo bioavailability of CsA. From these findings, the LHPs, with the advantage of avoiding alveolar macrophage clearance, could be a viable choice for delivering CsA by inhalation administration relative to oral administration.

show abstract

Section: Resultsmentioning

confidence: 99%

Development of Large Hollow Particles for Pulmonary Delivery of Cyclosporine A

Huang,

Tang,

Meng

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…The formulation NT5 comprised of HPMC K100, and PVP K30 was discovered to have a hardness of 4.2 kg/cm 2 . Due to its strong and viscous gel layer, HPMC is frequently used for the preparation of hydrophilic matrix gels [ 22 ]. This layer shields the matrix from rapid disintegration, and it regulates the rate of drug release without altering the release profile.…”

Section: Resultsmentioning

confidence: 99%

Development and Characterization of Gel-Based Buccoadhesive Bilayer Formulation of Nifedipine

Alagusundaram,

Jain,

Begum

et al. 2023

Gels

View full text Add to dashboard Cite

A promising controlled drug delivery system has been developed based on polymeric buccoadhesive bilayered formulation that uses a drug-free backing layer and a polymeric hydrophilic gel buccoadhesive core layer containing nifedipine. The DSC thermogravimetric analysis confirms the drug’s entrapment in the gel layer and reveals no evidence of a potential interaction. Various ratios of bioadhesive polymers, including HPMC K100, PVP K30, SCMC, and CP 934, were combined with EC as an impermeable backing layer to ensure unidirectional drug release towards the buccal mucosa. The polymeric compositions of hydrophilic gel-natured HPMC, SCMC, and CP formed a matrix layer by surrounding the core nifedipine during compression. Preformulation studies were performed for all of the ingredients in order to evaluate their physical and flow characteristics. Ex vivo buccoadhesive strength, surface pH, swelling index, in vitro and in vivo drug release, and ex vivo permeation investigations were performed to evaluate the produced gel-based system. Rapid temperature variations had no appreciable impact on the substance’s physical properties, pharmacological content, or buccoadhesive strength during stability testing using actual human saliva. It was clear from a histological examination of the ex vivo mucosa that the developed system did not cause any irritation or inflammation at the site of administration. The formulation NT5 was the best one, with a correlation coefficient of 0.9966. The in vitro and in vivo drug release profiles were well correlated, and they mimic the in vitro drug release pattern via the biological membrane. Thus, the developed gel-based formulation was found to be novel, stable, and useful for the targeted delivery of nifedipine.

show abstract

“…Poloxamer 407 has thermo-sensitivity, usually used in dental surgery [46]. HPMC is usually used as a drug tablet or soft gel capsule as a controlled release matrix [47,48]. All materials were prepared by mixing immediately prior to use while maintaining sterility.…”

Section: Preparation Of the Composite Carriermentioning

confidence: 99%

Concentration-Dependent Efficacy of Recombinant Human Bone Morphogenetic Protein-2 Using a HA/β-TCP Hydrogel Carrier in a Mini-Pig Vertebral Oblique Lateral Interbody Fusion Model

Lee

Kang

Lee

et al. 2023

IJMS

View full text Add to dashboard Cite

Bone morphogenetic protein-2 (BMP-2) is used in the treatment of degenerative spinal disease and vertebral fractures, spine fusion, dental surgery, and facial surgery. However, high doses are associated with side effects such as inflammation and osteophytes. In this study, we performed spinal fusion surgery on mini-pigs using BMP-2 and a HA/β-TCP hydrogel carrier, and evaluated the degree of fusion and osteophyte growth according to time and dosage. Increasing the dose of BMP-2 led to a significantly higher fusion rate than was observed in the control group, and there was no significant difference between the 8-week and 16-week samples. We also found that the HA + β-TCP hydrogel combination helped maintain the rate of BMP-2 release. In conclusion, the BMP-2-loaded HA/β-TCP hydrogel carrier used in this study overcame the drawback of potentially causing side effects when used at high concentrations by enabling the sustained release of BMP-2. This method is also highly efficient, since it provides mineral matter to accelerate the fusion rate of the spine and improve bone quality.

show abstract

Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug

Cited by 14 publications

References 49 publications

Development of Large Hollow Particles for Pulmonary Delivery of Cyclosporine A

Development of Large Hollow Particles for Pulmonary Delivery of Cyclosporine A

Development and Characterization of Gel-Based Buccoadhesive Bilayer Formulation of Nifedipine

Concentration-Dependent Efficacy of Recombinant Human Bone Morphogenetic Protein-2 Using a HA/β-TCP Hydrogel Carrier in a Mini-Pig Vertebral Oblique Lateral Interbody Fusion Model

Contact Info

Product

Resources

About