Inhaled bosentan microparticles for the treatment of monocrotaline-induced pulmonary arterial hypertension in rats

Lee, Hyo‐Jung; Kwon, Yong-Bin; Kang, Ji‐Houn; Oh, Dong-Won; Park, Eun-Seok; Rhee, Yun-Seok; Kim, Ju‐Young; Shin, Dae-Hwan; Kim, Dong-Wook; Park, Chun‐Woong

doi:10.1016/j.jconrel.2020.08.050

Cited by 13 publications

(10 citation statements)

References 52 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In this study, raw lidocaine, petr MCT oil, GMS, and prepared ointments were analyzed. The spectrum of raw li was similar to that of the reference, showing absorption peaks at 3044, 2945, and 1 (Figure 3A) [49]. The shape of the droplet of the diluted ointment was confirmed by TEM (Figure 4).…”

Section: Physicochemical Characterization Of Lidocaine Ointmentmentioning

confidence: 52%

“…In this study, raw lidocaine, petrolatum, MCT oil, GMS, and prepared ointments were analyzed. The spectrum of raw lidocaine was similar to that of the reference, showing absorption peaks at 3044, 2945, and 1670 cm −1 (Figure 3A) [49]. Raman spectroscopy analysis can provide further confirmation of the stabi crystallinity of the prepared lidocaine ointments.…”

Section: Physicochemical Characterization Of Lidocaine Ointmentmentioning

confidence: 55%

See 1 more Smart Citation

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

Self Cite

View full text Add to dashboard Cite

Lidocaine, a commonly used local anesthetic, has recently been developed into a number of ointment products to treat hemorrhoids. This study examined its efficient delivery to the dermis through the pharmaceutical improvement of hemorrhoid treatment ointments. We attempted to increase the amount of skin deposition of lidocaine by forming a nanoemulsion through the self-nanoemulsifying effect that occurs when glycerol monostearate (GMS) is saturated with water. Using Raman mapping, the depth of penetration of lidocaine was visualized and confirmed, and the local anesthetic effect was evaluated via an in vivo tail-flick test. Evaluation of the physicochemical properties confirmed that lidocaine was amorphous and evenly dispersed in the ointment. The in vitro dissolution test confirmed that the nanoemulsifying effect of GMS accelerated the release of the drug from the ointment. At a specific concentration of GMS, lidocaine penetrated deeper into the dermis; the in vitro permeation test showed similar results. When compared with reference product A in the tail-flick test, the L5 and L6 compounds containing GMS had a significantly higher anesthetic effect. Altogether, the self-nanoemulsifying effect of GMS accelerated the release of lidocaine from the ointment. The compound with 5% GMS, the lowest concentration that saturated the dermis, was deemed most appropriate.

show abstract

Section: Physicochemical Characterization Of Lidocaine Ointmentmentioning

confidence: 52%

Section: Physicochemical Characterization Of Lidocaine Ointmentmentioning

confidence: 55%

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

Self Cite

View full text Add to dashboard Cite

show abstract

“…For the final physicochemical characterization, FT-IR spectra are shown in Figure 2 C. The spectrum of raw NFM showed strong infrared absorption at 1740–1680 cm −1 . These peaks correspond to C–H bonds [ 20 ], and broad infrared absorption at 3440–3000 cm −1 corresponds to N-H bonds [ 47 ] of guanidine and amidine groups. In the case of SD-NFM, although it shows a peak similar to the main peaks of raw NFM, the peak is weakened and broadened.…”

Section: Resultsmentioning

confidence: 99%

“…Based on the United States Pharmacopeia (USP) Chapter 601 specification of aerosols, the aerosol performance of the SD-NLMs DPI was determined using an 8-stage non-viable ACI (TE-20-800, TISCH Environmental, Cleves, OH, USA) and RS01 ® (Plastiape, Osnago, Italy). To prevent particle bouncing and re-entrainment, the collection plates of the ACI stage were pre-coated with silicone oil [ 20 ]. SD-NLMs equivalent to 10 mg of formulation were loaded into a hydroxypropyl methylcellulose hard capsule (HPMC, size 3).…”

Section: Methodsmentioning

confidence: 99%

“…Therefore, to treat and prevent SARS-CoV-2 using NFM, it is necessary to administer the drug via the respiratory tract, which is one of the routes of viral invasion and has a lower esterase level than the blood [ 19 ]. When the drug is administered via the respiratory tract, it results in high efficacy and reduced incidence of side effects [ 20 , 21 , 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats

et al. 2021

Self Cite

View full text Add to dashboard Cite

Coronavirus disease 2019 (COVID-19), caused by a new strain of coronavirus called severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is spreading rapidly worldwide. Nafamostat mesylate (NFM) suppresses transmembrane serine protease 2 and SARS-CoV-2 S protein-mediated fusion. In this study, pharmacokinetics and lung distribution of NFM, administered via intravenous and intratracheal routes, were determined using high performance liquid chromatography analysis of blood plasma, lung lumen using bronchoalveolar lavage fluid, and lung tissue. Intratracheal administration had higher drug delivery and longer residual time in the lung lumen and tissue, which are the main sites of action, than intravenous administration. We confirmed the effect of lecithin as a stabilizer through an ex vivo stability test. Lecithin acts as an inhibitor of carboxylesterase and delays NFM decomposition. We prepared inhalable microparticles with NFM, lecithin, and mannitol via the co-spray method. The formulation prepared using an NFM:lecithin:mannitol ratio of 1:1:100 had a small particle size and excellent aerodynamic performance. Spray dried microparticles containing NFM, lecithin, and mannitol (1:1:100) had the longest residual time in the lung tissue. In conclusion, NFM-inhalable microparticles were prepared and confirmed to be delivered into the respiratory tract, such as lung lumen and lung tissue, through in vitro and in vivo evaluations.

show abstract

Nanomedicine-based treatment: An emerging therapeutical strategy for pulmonary hypertension

et al. 2023

View full text Add to dashboard Cite

Inhaled bosentan microparticles for the treatment of monocrotaline-induced pulmonary arterial hypertension in rats

Cited by 13 publications

References 52 publications

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats

Nanomedicine-based treatment: An emerging therapeutical strategy for pulmonary hypertension

Contact Info

Product

Resources

About