ABSTRACT
Two male patients aged 33 and 38 years with mitochondrial encephalopathy with lactic acidosis and stroke-like episodes (MELAS)admitted in our hospital in 2016 and 2017 were reported.The main symptoms included abdominal pain and distension,numbness and weakness of the limbs.MRI showed mild ventriculomegaly with deepened sulcus and widened cerebral fissure,deepened bilateral cerebellar sulcus and the widened cleavage,atrophy of cerebellum and brainstem,and manifestations of acute cerebral infarction.Gene analysis showed mutation of mitochondrial DNA(mtDNA) A3243G.After definite diagnosis was made,patients reveived coenzyme Q10,ATP and vitamin supplements for improving circulation,and neurotrophic drugs for symptomatic treatment.The symptoms were slightly improved after treatment and two cases were followed-up as outpatients.
ABSTRACT
Ketoprofen, a non-steroidal anti-inflammatory drug with well-known anti-inflammatory, antipyretic and analgesic properties, has low solubility in water and causes local or systemic disturbance in the gastrointestinal tract. In the present study we investigated the potential of polyamidoamine (PAMAM) dendrimers as drug carriers of ketoprofen by in vitro and in vivo studies. The in vitro release of ketoprofen from the drug-dendrimer complex is significantly slower compared to pure ketoprofen. Anti-nociceptive studies using the acetic acid-induced writhing model in mice showed a prolonged pharmacodynamic behavior for the ketoprofen-PAMAM dendrimer complex. Also, the blood level studies were investigated. We concluded that PAMAM dendrimers might be considered as a potential drug carrier of ketoprofen with a sustained release behavior under suitable conditions.
Subject(s)
Dendrimers/administration & dosage , Drug Carriers/chemistry , Ketoprofen/administration & dosage , Ketoprofen/pharmacokinetics , Animals , Ketoprofen/pharmacology , Mice , Time FactorsABSTRACT
In the present study we investigated the effect of ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimers on the aqueous solubility of nicotinic acid. The aqueous solubility of nicotinic acid was measured in the presence of dendrimers at room temperature in distilled water. The effect of variables, such as pH condition, concentration, surface functional group and generation (molecule size) of dendrimer, has been investigated. Results showed that the solubility of nicotinic acid in the dendrimer solutions was proportional to dendrimer concentration, both amine and ester-terminated dendrimers caused the higher increase in nicotinic acid solubility at higher pH conditions. The order in which the dendrimers increased the solubility at a constant pH condition was G4>G3>G2>G1. In addition, at each pH, the solubility of nicotinic acid was greater in the presence of amine-terminated dendrimers compared to the amine ester-terminated dendrimers possessing the same number of surface functional groups. Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of nicotinic acid.
Subject(s)
Dendrimers/chemistry , Niacin/chemistry , Polyamines/chemistry , Ethylenediamines/chemistry , Hydrogen-Ion Concentration , Molecular Structure , Solubility , Solutions/chemistry , Structure-Activity Relationship , Surface PropertiesABSTRACT
Ketoprofen is a non-steroidal anti-inflammatory drug which is not freely soluble in water and creates gastrointestinal problems. In the present study we investigated the potential of polyamidoamine (PAMAM) dendrimers to increase the solubility of ketoprofen. The effect of variables, such as pH condition, concentration and generation of dendrimer, has been investigated. The experimental results showed that the solubility of ketoprofen in the dendrimer solutions was proportional to dendrimer concentration. Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of ketoprofen.
Subject(s)
Dendrimers/chemistry , Ketoprofen/chemistry , Polyamines/chemistry , Hydrogen-Ion Concentration , Molecular Structure , Solubility , Solutions/chemistry , Structure-Activity Relationship , Surface PropertiesABSTRACT
The aqueous solubility of non-steroidal anti-inflammatory drugs (NSAIDs) Ketoprofen, Ibuprofen, Diflunisal and Naproxen were measured in the presence of the ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimers at 37 degrees C. The effect of concentration and generation of the PAMAM dendrimers has been investigated. Results showed that the solubility of NSAIDs in the PAMAM dendrimer solutions was approximately proportional to dendrimer concentration; the solubility of NSAIDs in higher generation PAMAM solutions was in fact higher that those in lower ones; the order of increased solubility of NSAIDs in PAMAM dendrimers at a constant dendrimer concentration and generation was Naproxen>Ketoprofen>Ibuprofen>Diflunisal. Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of NSAIDs.
