Buccal Transmucosal Delivery System of Enalapril for Improved Cardiac Drug Delivery: Preparation and Characterization

Purpose: To prepare and characterize buccal transmucosal delivery system of enalapril maleate for overcoming its low bioavailability, and hence provide improved therapeutic efficacy and patient compliance.Methods: Transmucosal drug delivery systems of enalapril maleate were formulated as buccal films by solvent casting technique using polyvinylpyrrolidone K90, hydroxypropyl methylcellulose, sodium carboxymethylcellulose (high viscosity). The films were evaluated for film weight, thickness, folding endurance, drug content uniformity, surface pH, in vitro residence time, in vitro drug release and ex-vivo permeation.Results: All the formulations showed high drug content (96.45 to 98.49 %). Those with good swelling showed good residence time. In vitro drug release was highest for films prepared with high viscosity grade sodium carboxymethylcellulose (SCMC- HV,F2), releasing 92.24 % of drug in 1.5 h) followed by F4 (containing polyvinyl pyrrolidone K-90 1 % w/v and SCMC (HV) 1 % w/v). Ex-vivo drug permeation at the end of 10 h was 82.24 and 89.9 % for F2 and F4, respectively.Conclusion: Prompt drug release was obtained from the formulation (F2) containing SCMC 2 % w/v with 10 mg enalapril. However, on the basis of the highest swelling and residence time, and controlled drug release, formulation F4 (containing PVP K-90 and SCMC HV) would be suitable for the development of buccal film for effective therapy of cardiac diseases.Keywords: Cardiac disease, Transmucosal, Buccal films, Enalapril maleate, Drug release, Ex-vivo permeatio

3′,6′-Bis(ethyl­amino)-2′,7′-dimethyl-2-{2-(E)-[(thio­phen-2-yl)methyl­idene­amino]­eth­yl}spiro­[isoindoline-1,9′-xanthen]-3-one methanol monosolvate

The title compound, C33H34N4O2S·CH3OH, was prepared as a spiro­lactam ring formation of rhodamine 6 G dye for comparison with a ring-opened form. The xanthene and spiro­lactam rings are approximately planar [r.m.s. deviations from planarity = 0.122 (3) and 0.072 (6) Å, respectively]. The dihedral angles formed by the spiro­lactam and thio­phene rings with the xanthene ring system are 89.7 (6) and 86.5 (2)°, respectively. The crystal structure features N—H⋯O and C—H⋯O hydrogen bonds

Comparison of survival, acute toxicities, and dose-volume parameters between intensity-modulated radiotherapy with or without internal target volume delineation method and three-dimensional conformal radiotherapy in cervical cancer patients:A retrospective and propensity score-matched analysis

BACKGROUND: To evaluate whether the use of the internal target volume (ITV) delineation method improves the performance of intensity‐modulated radiotherapy (IMRT) and three‐dimensional conformal radiotherapy (3DCRT) in terms of survival, acute toxicities, and dose–volume parameters. METHODS: A total number of 477 cervical cancer patients who received concurrent chemoradiotherapy (CCRT) from January 2012 to December 2016 were retrospectively analyzed. They were divided into four groups: the non‐ITV (N‐ITV) + IMRT, ITV + IMRT, N‐ITV + 3DCRT, and ITV + 3DCRT groups, with 76, 41, 327, and 33 patients, respectively. Survival analysis was performed with the Kaplan–Meier and the log‐rank tests, and acute toxicity analysis was performed with the chi‐squared test and the binary logistic regression test. Using the propensity score matching (PSM) method, 92 patients were matched among the four groups, and their dose–volume parameters were assessed with the Kruskal–Wallis method. RESULTS: The median follow‐up time was 49 months (1–119) for overall survival (OS). The 5‐year OS rate was 66.4%. The ITV delineation method was an independent prognostic factor for OS (HR [95% CI]: 0.52 [0.27, 0.98], p = 0.044) and progression‐free survival (PFS) (HR [95% CI]: 0.59 [0.36, 0.99], p = 0.045). The ITV + IMRT group had the lowest incidence rate (22%) and the N‐ITV + IMRT group had the highest incidence rate of grade ≥3 hematological toxicity (HT) (46.1%) among the four groups. The pelvic bone marrow relative V10, V20, and V30 in the N‐ITV + IMRT group was higher than those in the ITV + IMRT and N‐ITV + 3DCRT groups (p < 0.05). CONCLUSIONS: The use of ITV for IMRT treatment planning was associated with improved overall survival and progression‐free survival, with lower HT rate

Manipulating spatial structure of high-order quantum coherence with entangled photons

High-order quantum coherence reveals the statistical correlation of quantum particles. Manipulation of quantum coherence of light in temporal domain enables to produce single-photon source, which has become one of the most important quantum resources. High-order quantum coherence in spatial domain plays a crucial role in a variety of applications, such as quantum imaging, holography and microscopy. However, the active control of high-order spatial quantum coherence remains a challenging task. Here we predict theoretically and demonstrate experimentally the first active manipulation of high-order spatial quantum coherence by mapping the entanglement of spatially structured photons. Our results not only enable to inject new strength into current applications, but also provide new possibilities towards more wide applications of high-order quantum coherence.Comment: 11 pages, 5 figure