Indian scientists have provided a new lease of life to the arthritis medicine sulfapyridine by employing an innovative drug delivery method to take away its side effects.
Sulfapyridine is the third oldest drug still in use in the remedy of rheumatoid arthritis, an autoimmune inflammatory joint disease, according to the researchers from Lovely Professional University (LPU) in Punjab.
Alternatively, long term use of the drug leads to side effects such as nausea or vomiting, rashes, dizziness, anxiety and abdominal pain, they said.
“As the molecule has side effect because of its higher dose, we developed a formulation which will also be delivered directly to the site of action and thus is protected,” said Bhupinder Kapoor, Associate Professor, School of Pharmaceutical Sciences, LPU, told PTI.
In their study published in the peer-reviewed publication ‘Materials Science and Engineering C’, the researchers reported developing a prodrug of sulfapyridine and then incorporated it into an innovative delivery system.
The prodrug exhibited better retention in liposomes, as in comparison to the drug, thus reducing the symptoms of inflammation.
Liposomes are spherical vesicles having no less than one lipid bilayer which are used as a vehicle for administration of pharmaceutical drugs.
The prodrug remedy is administered by injecting the affected area of the patient, and not through oral consumption, according to the researchers.
Because of this the medication only remains in the affected area, without spreading to the remainder of the body, they said.
The research team, including Kapoor, Monica Gulati and Sachin K. Singh from LPU, successfully conducted the pre-clinical trials in addition to the testing of the drug delivery mechanism.
“We conducted a study to understand the efficacy of sulfapyridine-derived liposomes. In arthritic rats, prodrug liposomes were found to reverse the symptoms of inflammation, including the levels of biochemical markers,” Kapoor explained.
“Due to this fact, liposomes of bio-responsive prodrugs offer a revolutionary approach in the remedy of rheumatoid arthritis,” he said.
The study used to be carried in collaboration with researchers at Fortis Hospital, Ludhiana & JSS College of Pharmacy, Ooty, Tamil Nadu.
Calling the result of the study as “promising”, Dr. Arup Kumar Banerjee from North Bengal Medical College and Hospital in Siliguri, West Bengal famous that prodrugs are compounds, or a derivative of a drug, that themselves are pharmacologically inactive but after administration get metabolised in the body into its active form.
“Prodrug form increases the bioavailability of the particular drug by defying metabolism in site other than the intended one and also decreases the adverse side effect by selective absorption or metabolism at the target cells or organs,” Banerjee, who used to be not involved in the study, told PTI.
Around 10 per cent of all drugs being used today are administered in the body in prodrug form, he added.
At present sulfapyridine is used in the form of sulfasalazine which is really useful orally in high dose and has few side effects because of exposure to nontarget sites, the researchers said.
For the successful retention of the drug at the injection site, they synthesised its lipophilic prodrug which is retained in the injection site for a longer time frame and required in very low dose, due to this fact has no side effects and dosing frequency could also be very less.
As sulfapyridine isn’t a suitable molecule because of bad solubility, the researchers synthesised its prodrug which will also be retained in injection site for a longer time frame, and due to this fact is effective in very low dose and without any side effect.
The researchers said their prodrug will need approval for sales and marketing from India’s drug regulatory body.
The team has filed for a patent, and the pre-evaluation phase is now total. They’re also applying for an international patent for this new drug delivery method.
(This story has been published from a wire agency feed without modifications to the text.)
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