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Cancer-targeted PDC Discovery

Phospholipid drug conjugate is another form of drug delivery system that is extensively applied for various anti-cancer studies. As a biological company dedicated to human health research, Creative Biolabs has committed to cancer-targeted researches many years ago. We have absolute advantages in providing the first-class products and related services about applications of the phospholipid drug conjugate.

Background of PDC

Phospholipid drug conjugate (PDC), also known as phospholipid-based prodrug, refers to a newly important class of therapeutic agents or pro-drugs, formed by one or more pharmaceutical molecules covalently bound to a specific phospholipid, which is a kind of bioreversible derivatives of active drug molecules with the potential to improve some physiological barriers. The PDC approach is mainly associated with targeting the phospholipase A2 enzyme, which specifically hydrolyzes the sn-2 fatty acyl bond of phospholipid with arachidonic acid and lysophosphatidic acid release. The design of the drug moiety covalently attached to the sn-2 position of a phosphate group is proposed to avoid the hydrolysis, thereby enabling the PDCs to be absorbed into the metabolic phospholipid processing pathways.

PDCs have received much attention in the past few decades and have been widely studied and applied as new targeted therapies, mainly due to their outstanding advantages and ease of synthesis and production. Compared with other lipid-based drug delivery systems like liposomes, lipid particulate, and lipid-core micelles, PDCs are more flexible in structure with higher drug loading, specificity, and permeability, which show the potential to develop promising and targeting therapeutic agents in clinics.

Fig.1 Characteristics of PDCs. (Markovic, Milica, et al, 2018) Fig.1 Characteristics of PDCs (Markovic, 2018).

Cancer-targeted PDC Discovery

Modern novel drug delivery systems or cancer treatments mainly focus on improving the non-specific deficiency of current therapies like chemotherapeutics, ie, targeted drug release rather than non-site avoidance. As one of the novel lipid-based drug carriers, PDC is another brilliant targeted treatment candidate, particularly for cancer therapy in recent years. Unlike lipid-based drug particulates, cancer-targeted therapies of PDCs are realized by covalent modification of the drugs with phospholipids and different specific molecules. Generally, tumor cell differs from the healthy cell in that plasma membranes of cancer cells have a higher level of lipid rafts and overexpressed phospholipase A2. PDCs are more susceptible to be taken up by lipid raft microdomains expressed on tumor cells, where PDCs may be activated by phospholipase A2 and release the free anti-tumor drugs.

Fig.2 llustration of PL-drug conjugates activation in the sPLA2 overexpressing tissues. (Markovic, Milica, et al, 2018) Fig.2 llustration of PL-drug conjugates activation in the sPLA2 overexpressing tissues (Markovic, 2018).

Chose Us for Your Cancer-targeted PDC Discovery

Creative Biolabs is a leading biological company and service provider that focuses on the development of human health. Experienced in both cancer treatment and novel drug delivery systems, we can apply our specific phospholipid drug conjugates products for different cancer treatment research.

In addition to phospholipid drug conjugates, Creative Biolabs also provides other various services on liposome development. Please feel free to contact us for more information and a detailed quote.

Reference:

  1. Markovic, M.; et al. Prospects and Challenges of Phospholipid-Based Prodrugs. Pharmaceutics. 2018, 10(4): pii, E210.
For Research Use Only. Not For Clinical Use