Sepideh Mahinrousta, Heidar Sharafi, Seyed Moayed Alavian, Bita Behnava, Ali Pouryasin,
Volume 15, Issue 7 (12-2012)
Abstract
Background: Nucleos(t)ide analogues, such as lamivudine and adefovir, are effective drugs for treatment of hepatitis B patients. However, long-term treatment with these drugs leads to the emergence of the nucleos(t)ide analogue resistant strains. The impact of nucleos(t)ide analogues on the emergence of HBsAg escape mutations is not clarified. Hence, the aim of this study was to determine HBsAg escape mutations in chronic hepatitis B patients treated with nucleos(t)ide analogues. Materials and Methods:A cross-sectional study was performed on 50 patients with chronic hepatitis B under treatment with nucleos(t)ide analogues (lamivudine and/or adefovir) and 50 naive chronic hepatitis B patients. HBV DNA was extracted from plasma and S gene of virus was amplified by Nested-PCR followed by direct sequencing. HBsAg gene sequence of the samples was evaluated for detection of HBsAg escape mutations. Results: Among the 100 patients, the following HBsAg escape mutations were identified: sQ101H, sG119R, sP120S, sP127S, sA128V, sG130N, sG130R, sT131I, sM133I, and sY134N. The frequency of HBsAg escape mutations in patients under treatment of nucleos(t)ide analogues was 16% and in naïve patients was 6% (p=0.2, OR=2.98). Conclusion:According to the obtained results, there seems to be no association between using nucleos(t)ide analogues and emergence of HBsAg escape mutations.
Hosein Heydari , Mehdi Shafiee Ardestani, Rezvan Zabihollahi, Seyed Mehdi Sadat , Shiva Irani , Seyed Nezamedin Hoseini, Safieh Amini, Seyed Davar Syadat, Mohammad Sadegh Khosravi, Alireza Azizi Saraji, Pouneh Rahimi, Mohammad Reza Aghasadeghi,
Volume 16, Issue 6 (9-2013)
Abstract
Background: Due to the lack of efficient anti-HIV vaccine, anti-HIV pharmaceuticals play an important role in controlling HIV infection. Also significant rise in drug resistance and drug toxicity has caused increased interest in finding new anti-HIV agents. In this study, a nano-sized version of lamivudine based on PEGylated chitosan was synthesized.
Materials and Methods: In this research, nanoparticles of chitosan were efficiently PEGylated for increasing their stability in water and then the anti-HIV drug, lamivudine, was loaded on these PEGylated nanoparticles. After purification and lyophilization of new synthesized nanoparticle, the raw materials and final product were sampled and FTIR, HNMR and CHN analyses were done.
Results: Results of HNMR spectroscopy showed that chitosan nanoparticle was successfully PEGylated. HNMR data confirmed FTIR results and indicated that lamivudine was conjugated on chitosan nanoparticle. In addition, CHN analysis data also confirmed both HNMR and FTIR data, and demonstrated that a high yield of chitosan nanoparticle PEGylation (approximately 97%) was done and illustrated a high capacity of lamivudine conjugation on nano-sized PEGylated chitosan (30% W/W chitosan).
Conclusion: In this study, lamivudine drug was successfully synthesized, based on PEGylated chitosan nanoparticle.
