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1.
Adv Exp Med Biol ; 1391: 137-159, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36472821

RESUMO

Infertility is a universal health problem affecting 15% of couples, out of which 20-30% cases are due to male infertility. The leading causes of male infertility include hormonal defects, physical reasons, sexual problems, hazardous environment, stressful lifestyle, genetic factors, epigenetic factors, and oxidative stress. Various physiological functions involve reactive oxygen species (ROS) and nitrogen species at appropriate levels for proper smooth functioning. ROS control critical reproductive processes such as capacitation, acrosomal reaction, hyperactivation, egg penetration, and sperm head decondensation. The excessive free radicals or imbalance between ROS and endogenous antioxidant enzymes damages sperm membrane by inducing lipid peroxidation causing mitochondrial dysfunction and DNA damage that eventually lead to male infertility. Numerous synthetic products are available in the market to treat infertility problems, largely ending in side effects and repressing symptoms. Ayurveda contains a particular group of Rasayana herbs, called vajikarana, that deals with nourishment and stimulation of sexual tissues, improves male reproductive vitality, and deals with oxidative stress via antioxidant mechanism. The present study aims to describe oxidative stress and the role of herbal drugs in treating male infertility.


Assuntos
Infertilidade Masculina , Sêmen , Masculino , Humanos , Ayurveda , Epigenômica , Infertilidade Masculina/tratamento farmacológico , Estresse Oxidativo
2.
Drug Res (Stuttg) ; 71(4): 204-212, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33348390

RESUMO

OBJECTIVE: The present investigation entailed determination of effect of diverse cross-linking agents on Losartan Potassium loaded chitosan microspheres. The emulsion cross-linking method was employed to formulate the microspheres with an endeavour to achieve maximum sustained effect. METHODS: The FTIR studies revealed absence of any interaction between Losartan and chitosan. The emulsion cross linking method was accomplished in three steps encompassing formation of an aqueous and oily phase, emulsification and cross-linking. A total of eighteen Losartan formulations were developed using six different cross-linkers at three varying level were screened for optimum parameters. The in vitro drug release parameters of optimum formulations (LC3, LE3, LF3, LG3, LS3 and LV3) containing citric acid, epichlorohydrin, formaldehyde, glutaraldehyde, suphuric acid and vanillin as cross-linkers were assessed to determine the sustained effect. RESULTS: The values of evaluated parameters including percent yield (94.67%), average particle size (51.19 µm), drug content (44.38 mg) and entrapment efficiency (88.77%) connoted LG3 as the best formulation. Additionally, the values of relative measure of skewness (ß1=0.01 and γ1=0.10) and platykurtic (ß2=1.26) size distribution were least for LG3 with spherical shape and smooth surface as revealed by SEM studies. CONCLUSION: The outcome of in vitro release and other characterizations of microspheres explicitly revealed glutaraldehyde as the best cross-linker amongst the cross-linkers used herewith. The maximum sustained effect (lasting over a period of 24 h) accompanied with higher MDT and t50% with lower%DE and Q14h values thus corroborated the objective of attaining sustained release of Losartan.


Assuntos
Quitosana/química , Preparações de Ação Retardada/farmacocinética , Excipientes/química , Losartan/farmacocinética , Reagentes de Ligações Cruzadas/química , Preparações de Ação Retardada/química , Composição de Medicamentos , Liberação Controlada de Fármacos , Emulsões , Losartan/química , Microesferas , Tamanho da Partícula
3.
Acta Pharm ; 59(1): 1-13, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-19304554

RESUMO

The current study involves development of oral bioadhesive hydrophilic matrices of hydralazine hydrochloride, and optimization of their in vitro drug release profile and ex vivo bioadhesion against porcine gastric mucosa. A 32 central composite design was employed to systematically optimize the drug delivery formulations containing two polymers, viz., carbomer and hydroxypropyl methyl cellulose. Response surface plots were drawn and optimum formulations were selected by brute force searches. Validation of the formulation optimization study indicated a very high degree of prognostic ability. The study successfully undertook the development of an optimized once-a-day formulation of hydralazine with excellent bioadhesive and controlled release characteristics.


Assuntos
Portadores de Fármacos/química , Hidralazina/administração & dosagem , Vasodilatadores/administração & dosagem , Resinas Acrílicas/química , Adesividade , Administração Oral , Animais , Química Farmacêutica , Preparações de Ação Retardada , Mucosa Gástrica/metabolismo , Hidralazina/química , Derivados da Hipromelose , Técnicas In Vitro , Metilcelulose/análogos & derivados , Metilcelulose/química , Suínos , Comprimidos , Vasodilatadores/química
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