RESUMEN
Amphiphilic functional polycaprolactone (PCL) diblock copolymers are excellent candidates for micellar drug delivery. The functional groups on the backbone significantly affect the properties of PCL. A systematic investigation of the effect of aromatic substituents on the self-assembly of γ-functionalized PCLs and the delivery of doxorubicin (DOX) is presented in this work. Three thermoresponsive amphiphilic diblock copolymers with poly(γ-benzyloxy-ε-caprolactone) (PBnCL), poly(γ-phenyl- ε-caprolactone) (PPhCL), poly(γ-(4-ethoxyphenyl)-ε-caprolactone) (PEtOPhCL), respectively, as hydrophobic block and γ-tri(ethylene glycol) functionalized PCL (PME3CL) as hydrophilic block were prepared through ring-opening polymerization (ROP). The thermoresponsivity, thermodynamic stability, micelle size, morphology, DOX-loading, and release profile were determined. The LCST values of amphiphilic diblock copolymers PME3CL-b-PBnCL, PME3CL-b-PPhCL, and PME3CL-b-PEtOPhCL are 74.2°C, 43.3°C, and 37.3°C, respectively. All three copolymers formed spherical micelles in phosphate-buffered saline (PBS, 1×, pH = 7.4) at low concentrations ranging from 8.7 × 10-4 g/L to 8.9 × 10-4 g/L. PME3CL-b-PBnCL micelles showed the highest DOX loading capacity of 3.01 ± 0.18 (wt%) and the lowest drug release, while PME3CL-b-PEtOPhCL micelles exhibited the lowest DOX loading capacity of 1.95 ± 0.05 (wt%) and the highest drug release. Cytotoxicity and cellular uptake of all three micelles were assessed in vitro using MDA-MB-231 breast cancer cells. All three empty micelles did not show significant toxicity to the cells at concentrations high up to 0.5 mg/mL. All three DOX-loaded micelles were uptaken into the cells, and DOX was internalized into the nucleus of the cells.
RESUMEN
Costus afer (C. afer) is a plant commonly known as ginger lily, spiral ginger, or bush cane. It is reportedly used in traditional medicine practice (TMP) to treat and manage many ailments including diabetes mellitus, stomach ache, arthritis, inflammation, and gout. These purported ethnomedicinal uses have triggered many research studies on the plant to amass scientific evidence. However, these research reports are scattered, and thus, this systematic review seeks to provide a comprehensive update on it covering its traditional uses, phytochemical and nutritional constituents, pharmacological activities, and toxicological effects. An online search was done using search engines such as Google Scholar, PubMed, and ScienceDirect from the period 1970 to 2019. The online search included the use of keywords, "Costus afer Ker-Gawl" or "Costus afer." The search revealed that the stem and leaves of the plant contain substantial amounts of micronutrients and macronutrients. The leaves, stem, rhizomes, and roots of C. afer contain several steroidal sapogenins, aferosides, dioscin, and paryphyllin C and flavonoid glycoside kaempferol-3-O-α-L-rhamnopyranoside. Experimental studies on various parts of the plant showed bioactivities such as antihyperglycemic, hepatocellular protection, cardioprotection, nephroprotection, testicular protection, CNS depressant, analgesic, antiarthritis, antibacterial, and antioxidant. Based on these evident data, it is concluded that the plant could be used as an alternative and complementary therapy for many oxidative stress-related diseases, provided further scientific studies on the toxicological and pharmacological aspects are carried out.