Organic Chemistry Laboratory, Chemical Engineering Department, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Int J Pharm. 2011 May 16;409(1-2):216-28. doi: 10.1016/j.ijpharm.2011.02.004. Epub 2011 Feb 21.
Alkannin, shikonin (A/S) and their derivatives are naturally occurring hydroxynaphthoquinones with a well-established spectrum of wound healing, antimicrobial, anti-inflammatory, antioxidant and antitumor activity. Clinical studies over the years revealed that A/S derivatives-based wound healing preparations (such as HELIXDERM(®)) are among a very small group of therapeutics that modulate both the inflammatory and proliferative phases of wound healing and present significant tissue regenerative activity. The purpose of the present work was to combine the biological properties of A/S and the advantages of electrospun meshes to prepare a potent topical/transdermal biomaterial for A/S. Four biocompatible polymers (cellulose acetate, poly(L-lactide), poly(lactide-co-glycolide) LA/GA:50/50 and 75/25) were used for the first time, to produce electrospun fiber mats containing either shikonin or A/S mixture in various amounts. Both drugs were effectively loaded into the above biomaterials. The incorporation of drugs did not considerably affect fibers morphology and their mean diameter size varied from 315 to 670 nm. High drug entrapment efficiencies (ranged from 74% to 95%) and appropriate release profiles were achieved, that render these fibers as potential A/S topical/transdermal wound healing dressings. Given the multifunctional activity of the natural products alkannins and shikonins, their consideration as bioactive constituents for tissue engineering scaffolds seems a promising strategy for repairing and regenerating tissues and mainly skin.
白花丹素、紫草素(A/S)及其衍生物是天然存在的羟基萘醌,具有广泛的伤口愈合、抗菌、抗炎、抗氧化和抗肿瘤活性。多年的临床研究表明,基于 A/S 衍生物的伤口愈合制剂(如 HELIXDERM(®))是一小部分能够调节伤口愈合的炎症和增殖阶段并具有显著组织再生活性的治疗药物之一。本工作的目的是将 A/S 的生物学特性与电纺网的优势相结合,制备一种有效的局部/经皮 A/S 生物材料。首次使用四种生物相容性聚合物(醋酸纤维素、聚(L-丙交酯)、聚(丙交酯-乙交酯)LA/GA:50/50 和 75/25),以生产含有不同量紫草素或 A/S 混合物的电纺纤维垫。两种药物均能有效地负载到上述生物材料中。药物的掺入并没有显著影响纤维的形态,其平均直径大小从 315nm 到 670nm 不等。实现了高药物包封效率(74%至 95%)和适当的释放曲线,使这些纤维成为有潜力的 A/S 局部/经皮伤口愈合敷料。鉴于天然产物白花丹素和紫草素的多功能活性,将其作为组织工程支架的生物活性成分似乎是修复和再生组织,特别是皮肤的一种很有前途的策略。