Background Podophyllotoxin (PPT) is a naturally occurring compound obtained from the roots of Podophyllum species, indicated for a variety of malignant tumors such as breast, lung, and liver tumors. This toxic polyphenol (PPT) exhibited significant activity against P-glycoprotein (P-gp) mediated multidrug-resistant (MDR) cancer cells. However, extremely poor water solubility, a narrow therapeutic window, and high toxicity have greatly restricted the clinical uses of PPT. Therefore, the present research was aimed to synthesize the water-soluble ester prodrug of PPT with polyacrylic acid (PAA), a water-soluble polymer by Steglich esterification reaction, and to screen it for assay, solubility, in vitro hemolysis, in vitro release, and in vitro anticancer activity. Results The Fourier transform infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopy results revealed the successful synthesis of podophyllotoxin-polyacrylic acid conjugate (PPC). The assay and saturation solubility of the prodrug is found to be 64.01 ± 4.5% and 1.39 ± 0.05 mg/mL (PPT equivalent) respectively. The PPC showed CMC (critical micelle concentration) of 0.430 mg/mL in distilled water at room temperature. The PPC micelles showed a mean particle size of 215 ± 11 nm with polydispersity index (PDI) of 0.193 ± 0.006. Further, the transmission electron microscope (TEM) results confirmed the self-assembling character of PPC into micelles. The PPC caused significantly less hemolysis (18.6 ± 2.9%) than plain PPT solution. Also, it demonstrated significantly (p < 0.01) higher in vitro cytotoxicity against both sensitive as well as resistance human breast cancer cells (MCF-7 and MDA MB-231) after 48 h of treatment. Conclusion The obtained study results clearly revealed the notable in vitro anticancer activity of PPT following its esterification with PAA. However, further in vivo studies are needed to ascertain its efficacy against a variety of cancers.
Transdermal drug delivery systems (TDDS) are used to transfer medicines into the systemic circulation through the skin. (Trans)dermal patches are well-known pharmacological formulations that are applied to the skin’s surface for a variety of reasons, ranging from treating cutaneous diseases to achieving a systemic impact. Transdermal drug delivery (TDD) devices rely heavily on adhesives. In addition to the normal functional adhesive qualities, adhesives for TDD applications must be biocompatible with the skin, chemically compatible with the medication, and enable consistent, efficient drug administration. One of the most important components of a TDDS is the pressure-sensitive adhesive (PSA). PSA’s primary role is to aid patch adherence to the skin, but it also serves as a matrix for the medication and other excipients. As a result, PSA impacts other important quality aspects of the TDDS, such as drug distribution, flux through skin, and physical and chemical stability of the completed product, in addition to patch adherence. This article addresses transdermal drug delivery systems, their benefits and drawbacks, and their uses in pharmaceuticals, as well as providing detailed information on pressure sensitive adhesives.
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