Cancer is the second leading cause of death worldwide. The most common form of cancer is prostate cancer and is known to be a leading cause of death among men world over. The current cancer therapies encounter challenges like nonspecific systemic distribution of antitumor agents, inadequate drug concentrations reaching the tumor, and the toxic effects related to the chemotherapeutic drugs.
Prostate, lung, bronchus, colon and rectal cancer are known to be the most common forms of cancer. Though uncommon in Asian countries, the incidence is increasing even in India. A recent report showed that prostate cancer ranks 5th in incidence and 4th in cancer mortality for men in Mumbai, India. The incidence is increasing by 1% every year. Conventional anti-cancer drugs cause serious side effects and, at best, merely extend the patient's lifespan by few years. For example, doxorubicin causes damage to heart, Methotrexate causes liver damage and cisplatin is known to cause nephrotoxicity. Thus, there is a demand to utilize alternative concepts or approaches for the treatment of cancer.
Drugs derived from natural products make an enormous contribution to drug discovery today. Over 60% of approved chemotherapeutic agents and their sources are derived from natural compounds. More than 25% of drugs used during the last two decades are directly derived from plants, while the other 25% are chemically altered natural products. From approximately 250,000 higher plants, only 5-15% has ever been investigated for bioactive compounds.
Medicinal plants/herbs are known to be the most exclusive source of life saving drugs for a major population world over. They have been widely used for the treatment of diseases in traditional way for several generations. An interaction between traditional medicine and modern biotechnological tools is to be established towards new drug development. The strong evidences from epidemiological and experimental studies highlight the importance of compounds derived from plants “phytochemicals” to reduce the risk of cancer and also inhibit the development and spread of tumors in experimental animals. About 60% of the currently known anticancer drugs are either directly derived from natural source or are chemically altered natural products. The advantage of using such compounds for cancer treatment is their relatively non-toxic nature and less side effects.
Pentacyclic triterpenes are secondary plant metabolites present widely in fruit peel, leaves and stem bark and other. These triterpenes display various pharmacological effects being devoid of prominent toxicity. Lupeol, a triterpene is an anti-oxidant, anti-mutagenic compound having anti-inflammatory effects in in vitro and in vivo systems. Lupeol is also known to induce differentiation and inhibit the cell growth of mouse melanoma and human leukemia cells. Lupeol and its ester are shown to have a protective effect against cyclophosphamide induced cardiac damage by restoration of mitochondrial structure and function. It has also been shown that lupeol activates Fas receptor mediated apoptotic machinery of LNCaP cells and inhibits the tumorigenesis of prostate cancer cells in an animal model.
However, an increase in the efficacy and bioavailability of these compounds remain a major drawback due to the lack of efficient delivery systems. Thus, the present disclosure aims at overcoming the drawbacks of the prior art to increase the efficacy and bioavailability of bioactive molecules/drugs.