Development and Characterization of PCL Electrospun Membrane-Coated Bletilla striata Polysaccharide-Based Gastroretentive Drug Delivery System.

The purpose of this study was to investigate the potential of Bletilla striata polysaccharide (BSP, a natural glucomannan material) for the development of a gastroretentive drug delivery system for the first time. Novel BSP-based porous wafer was prepared for levofloxacin hydrochloride (LFH) delivery by combining floating, swelling, and mucoadhesion mechanisms. The influences of BSP and ethyl cellulose (EC) on drug release and mucoadhesive strength were studied by 32 factorial design. The optimized matrix was coated with polycaprolactone (PCL) electrospun membrane by electrospinning and heat treatment technology. The optimized formula (F6, coated) exhibited Q4 h of 41.20 ± 1.90%, Q8 h of 76.49 ± 1.69%, and mucoadhesive strength of 86.11 ± 1.33 gf, and its drug release profile most closely resembled the Korsmeyer-Peppas model with anomalous diffusion driving mechanism. F6 (coated) also presented excellent buoyancy, preferred swelling characteristic due to the porous structure formed by freeze-drying. Meanwhile, the internal morphology, physical state, drug-excipient compatibility, and thermal behavior were recorded. The negligible cytotoxicity of F6 (coated) was observed in human gastric epithelial cell cultures. In the in vitro antimicrobial experiment, the prepared wafer exhibited obvious bacterial inhibition zone, and due to its longer gastric retention, the wafer also performed a more effective Helicobacter pylori clearance than free LFH in vivo. Graphical abstract.

Polysaccharides from tubers of Bletilla striata: Physicochemical characterization, formulation of buccoadhesive wafers and preliminary study on treating oral ulcer.

The purpose of this research is to arouse people's cognition of the dual role of Bletilla striata polysaccharide (BSP)-a kind of biocompatible, biodegradable natural biological materials with myriad pharmacological activities. BSP was extracted and characterized firstly. The results indicated that BSP was composed of mannose and glucose. The backbone of BSP mainly consisted of (1 → 4)-linked ß-D-mannopyranose. Afterwards, A 32 factorial design was employed for optimization of lyophilized wafers for the treatment of traumatic oral ulcer with concentrations of BSP and glycerin as independent variables. Tensile strength, mucoadhesive strength, and swelling index were measured as response variables. It was determined that the wafer prepared from a solution containing 4% (w/v) BSP and 7% (w/v) glycerin was the optimal formulation. The wafers exhibited sufficient mechanical strength and suitable surface pH. Morphology of the wafers was observed. DSC/TGA thermograms showed the presence of three peaks weight loss events and decomposition patterns. Moreover, in vivo examinations indicated that the BSP wafer significantly promoted ulcer healing at 7 days, while no statistically significant difference was observed on day 12. In conclusion, this study suggests that BSP is an ideal biomaterial for mucosal adhesion agents, playing a nontrivial role in promoting oral ulcer healing.

Novel Bletilla striata polysaccharide microneedles: Fabrication, characterization, and in vitro transcutaneous drug delivery.

Dissolving microneedles (MNs) have been widely studied for their applications in effective transdermal drug delivery due to their ability to dissolve within the skin. This study details the first reported successful preparation of novel dissolving MNs using Bletilla striata polysaccharide (BSP), a natural glucomannan material, and investigates the potential for using such MNs as a transdermal drug delivery vector. The prepared dissolving Bletilla striata polysaccharide microneedles (BMNs) had excellent moldability and were easily detached from the mold. Texture analysis and histological examination confirmed BMNs were strong enough to insert into the skin. The skin appeared slight irritation after removal of BMNs, but recovered within 24 h. Confocal laser scanning microscopy (CLSM) studies indicated that rhodamine B (RB) loaded in BMNs (as a model drug) could be gradually released, along with the dissolution of BSP in vivo, and then diffused from the insertion site to the periphery. Furthermore, we found that the RB-loaded BMNs could provide sustained drug release via the in vitro Franz cell experiment. These findings demonstrate that novel dissolving BMNs can be easily-manufactured, loaded with drug, and inserted into the skin for drug delivery.

In Vitro and In Vivo Antioxidant Activities of the Flowers and Leaves from Paeonia rockii and Identification of Their Antioxidant Constituents by UHPLC-ESI-HRMSn via Pre-Column DPPH Reaction.

The genus Paeonia, also known as the "King of Flowers" in China, is an important source of traditional Chinese medicine (TCM). Plants of this genus have been used to treat a range of cardiovascular and gynecological diseases. However, the potential pharmacological activity of one particular species, Paeonia rockii, has not been fully investigated. In the first part of the present study, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS), reducing power assays, and metal ion chelating assays were used to investigate the in vitro antioxidant activities of Paeonia rockii. In the second portion of the study, a mouse model of d-galactose-induced aging was used to validate the antioxidant effects of the flowers from Paeonia rockii in vivo. Lastly, potential antioxidant constituents were screened and identified by ultra-high pressure liquid chromatography and electrospray ionization coupled with high-resolution mass spectrometry (UHPLC-ESI-HRMSn) combined with the DPPH assay. Results indicated that the flowers and leaves exhibited stronger antioxidant activity than ascorbic acid in vitro. The therapeutic effect of Paeoniarockii was determined in relation to the levels of biochemical indicators, such as 8-iso-prostaglandin F2α (8-iso PGF2α) in the serum, superoxide dismutase (SOD), protein carbonyl, malondialdehyde (MDA), and glutathione (GSH) in the liver and brain, after daily intra-gastric administration of different concentrations of extracts (100, 200 and 400 mg/kg) for three weeks. The levels of 8-iso PGF2α (p < 0.01) and protein carbonyl groups (p < 0.01) were significantly reduced, whereas those of SOD (p < 0.05) had significantly increased, indicating that components of the flowers of Paeonia rockii had favorable antioxidant activities in vivo. Furthermore, UHPLC-ESI-HRMSn, combined with pre-column DPPH reaction, detected 25 potential antioxidant compounds. Of these, 18 compounds were tentatively identified, including 11 flavonoids, four phenolic acids, two tannins, and one monoterpene glycoside. This study concluded that the leaves and flowers from Paeonia rockii possess excellent antioxidant properties, highlighting their candidacy as "new" antioxidants, which can be utilized therapeutically to protect the body from diseases caused by oxidative stress.

Analytical Methods of Phytochemicals from the Genus Gentiana.

The genus Gentiana comprises approximately 400 species. Many species have a wide range of pharmacological activities and have been used therapeutically for thousands of years. To provide comprehensive guidance, utilization and quality control of Gentiana species, this review presents updated information concerning the recent application and progress of chemical analysis including phytochemical analysis, sample preparation and chemometrics. Detailed and comprehensive data including number of analytes, extraction/separation methods, analytical techniques and chemometrics are shown as corresponding tables. These data illustrate that the development of newly discovered compounds and therapeutic uses, understanding of the structure-activity relationship and establishment of harmonious and effective medicinal herb standards are the direction of advancement in future research.

Anti-inflammatory and Analgesic Effects of Polygonum orientale L. Extracts.

Background and Purpose:Polygonum orientale L. (family: Polygonaceae), named Hongcao in China, is a Traditional Chinese Medicinal and has long been used for rheumatic arthralgia and rheumatoid arthritis. However, no pharmacological and mechanism study to confirm these clinic effects have been published. In this investigation, the anti-inflammatory, analgesic effects and representative active ingredient compounds of P. orientale have been studied. Methods: Dried small pieces of the stems and leaves of P. orientale were decocted with water and partitioned successively to obtain ethyl acetate and ethyl ether extract of P. orientale (POEa and POEe). Chemical compositions of them were analyzed by UPLC-Q-Exactive HRMS. Anti-inflammatory and analgesic effects of POEa and POEe were evaluated using xylene induced ear edema, carrageenan induced paw edema, Freunds' complete adjuvant induced arthritis, and formaldehyde induced pain in rat. Their mechanisms of anti-inflammatory and analgesic effects were also studied via assays of TNF-α, IL-1ß, IL-6, and PGE2 in serum. Results: UPLC-Q-Exactive HRMS analysis showed that POEa and POEe mainly contained flavonoids including orientin, isoorientin, vitexin, luteolin, and quercetin. Furthermore, anti-inflammatory effects of POEa and POEe were evident in xylene induced ear edema. The paw edema in Freund's complete adjuvant and carrageenan were significantly (P < 0.05, 0.01) inhibited by POEa (5, 7.5 g/kg). POEe (7.5 g/kg) was significantly (P < 0.05, 0.01) inhibited Freunds' complete adjuvant induced paw edema and cotton pellet induced granuloma formation. Similarly, POEe significantly (P < 0.05, 0.01) inhibited the pain sensation in acetic acid induced writhing test. POEa (5, 7.5 g/kg) significantly (P < 0.05, 0.01) inhibited formaldehyde induced pain in both phases. POEa (7.5 g/kg) markedly (P < 0.05) prolonged the latency period of hot plate test after 30 and 60 min. The concentrations of TNF-α, IL-1ß, IL-6, and PGE2 were significantly (P < 0.01) decreased by POEa (3.75, 5 g/kg). Conclusion: POEa and POEe have anti-inflammatory and analgesic effects, which was mainly relevant to the presence of flavonoids, including orientin, isoorientin, vitexin, luteolin, and quercetin. The mechanism of anti-inflammatory and analgesic effects of POEa may be to decrease the concentrations of TNF-α, IL-1ß, IL-6, and PGE2 in serum.

In vivo wound healing and in vitro antioxidant activities of Bletilla striata phenolic extracts.

Bletilla striata has attracted extensive research interest due to the potential uses for its extracts to treat skin burns and inflammatory disorders in a clinical setting. My current research focuses on Bletilla striata polysaccharides (BSP), and often ignores the residues that remain after polysaccharide extraction. It also remains unclear whether the residues have medical value related its traditional clinic function. During this work, we firstly identified the contents of the post-extraction residue by UPLC-Q-Exactive Orbitrap-MS and evaluated its in vivo wound healing and in vitro antioxidant activity. The wound healing activity of the ointment containing residue was assessed for 15days the scald model was used in mice, followed by histopathology and histomorphological analysis. The in vitro antioxidant effect of Bletilla residue was researched using DPPH, ABTS, Hydroxyl radical scavenging, superoxideanion radical scavenging, and reducing power assays. AUPLC-Q-Exactive Orbitrap-MS analysis identified 6 phenolic compounds: protocatechuic acid, p-hydroxybenzoic acid, caffeic acid, p-hydroxybenzaldehyde, 3-Hydroxycinnamic acid, and ferulic acid. Animals treated with "mixed ointment" experienced inflammatory infiltration, which was lower than that of other groups. Both "BSPG ointment" and "Bletilla phenolic ointment" demonstrated superior tissue repair compared to the control. This study was the first to confirm that the residual liquid after polysaccharide extraction has excellent antioxidant and wound healing activities. In addition to Bletilla striata polysaccharides, the residual liquid can improve skin regeneration after burns and reduce inflammatory marker levels. These results have implications that the residual liquid has potential wound healing medicinal value.