Journal of Drug Delivery and Therapeutics (JDDT)
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Formulation Development and Evaluation of Sustained Release Ranolazine Microbeads using Natural Polymer
Get PDFThe goal of this study was to develop sustained-release microbeads containing Ranolazine. The Ranolazine was selected on the basis of its short half-life i.e., 1.5 h and used in treatment of Angina pectoris. The fundamental goal of this research is to increase duration of drug release. Ranolazine was encapsulated with natural polymers such as Hygrophila auriculata seed mucilage by an ionotropic gelation technique. The formulation batches were optimized with a 32 factorial design and physicochemical characteristics were also evaluated. The particle size of microbeads, entrapment efficiency of drug, surface morphology, In-vitro release of drug was investigated.
The in-vitro studies of optimized microbeads formulation batch (B2) containing 100:600 ratio of Hygrophila auriculata seed mucilage and sodium alginate exhibited as a sustained release of Ranolazine up to 12 h and. The mucoadhesion potential was found to be 97± 1% up 12 h. In our perspective, the current ER pellet formulation might be the most feasible alternative to traditional pain management formulas.
All the trial’s batches were shown to be suitable in extended release of a short elimination half-life medication with enhanced bioavailability, implying that it is useful for oral drug delivery.
Keywords: Design of experiment, Extrusion-spheronization, Ionic gelation, Microbeads, Ranolazine
Formulation and Evaluation of Sustained Release Tablet of Metformin by Ionic Gelation Technique using Sida acuta Gum as Release Retardant
Get PDFThis research was done to formulate and assess the sustained release property of metformin tablets prepared from metformin microcapsules produced by ionic gelation technique using Sida acuta gum or sodium carboxymethylcellulose as release retardant. Sida acuta gum was produced by isopropyl alcohol precipitation of the filtrate obtained from distilled water maceration of powdered dried Sida acuta leaves. Metformin and Sida acuta gum compatibility was determined using FTIR. Metformin microcapsules were prepared by ionic gelation technique using sodium alginate alone or with either Sida acuta gum or sodium carboxymethylcellulose as release retardant. The microcapsules were evaluated for % yield and flow properties. The size and surface morphology of the microcapsules were determined using scanning electron microscopy. Metformin tablets were prepared from the microcapsules using direct compression technique. The tablets were evaluated for hardness, friability and in vitro dissolution. There was no major incompatibility between metformin and Sida acuta gum. The microcapsules have excellent flow property and were of micrometer size range. They have rough surfaces. The friability of the tablets ranged from 0.4-1.6% while the hardness was from 3.82-11.17 Kgf. The tablets from formulations M2 failed both friability and hardness test. About 44.5-47.1% of metformin was released from the tablet formulations after 6 h while 86.0-100% was released after 10 h. All the tablet formulations showed sustained release ability.
Keywords: Microcapsules, metformin, Sida acuta gum, sustained release, ionic gelatio
Determination of Irinotecan enantiomer impurity in Irinotecan Hydrochloride API by using reverse-phase liquid chromatography
Get PDFTo evaluate and quantify Irinotecan (R-enantiomer) / Irinotecan related compound D in Irinotecan hydrochloride trihydrate API, a high stereo-specific liquid chromatography technique was developed and validated. The partition was accomplished on ChiralpakIC-3 (150 x 4.6 mm 3µm) through a mobile fragment comprising 0.1 % v/v Formic acid in water and acetonitrile with 1mL/min, 250C, 20µL, 50C and 370 nmas flow rate, column temparture, injection volume, sample cooler temperature and detection wavelength. At 8.903 and 9.75 min, the retention time of Irinotecan (R-enantiomer) and Irinotecan (S-enantiomer) was determined. The resolution between Irinotecan (R-enantiomer) and Irinotecan (S-enantiomer) was found to be 2.4. The impurity acceptance limit is 0.2 %. The established method\u27s precision, accuracy, sensitivity, linearity, specificity, and ruggedness were all verified in accordance with ICH recommendations. The qualifying sample LOQ was found to be 0.4 g/ml, while the minimal amount of sample needed for LOD detection was found to be 0.12 g/ml. The proposed reversed-phase method has been sophisticated and authenticated in accordance with ICH criteria and is capable of quantifying irinotecan enantiomer in irinotecan hydrochloride trihydrate API at trace level concentration. The specificity, linearity, and accuracy of the approach were used to guarantee its efficacy; as a result, it is appropriate for the task at hand, may be used successfully for routine laboratory analysis, and can be utilised for quality control.
Keywords: Irinotecan, liquid chromatography technique, enantiomer impurit
Comparative Spermatogenesis Activity of Eranda Moola (Ricinus Communis) Collected In Different Seasons as per Dravya Samgrahana Kaala: An Experimental Study
Get PDFIntroduction: Dravya sangrahana is one of the criteria where different seasons are indicated for collecting different parts of the plants. As per ancient drug collection practice roots are to be collected in Hemanth-Shishira (winter) or Greeshma rutu(summer). Eranda(Ricinus communis) is an important medicinal plant roots of which are particularly indicated as Vrishya (spermatogenic). Hence study has been planned to conduct a comparative spermatogenic activity of Ernadamoola collected in Greeshma rutu and Pravarat rutu and Shishsira ritu. Materials and methods: Roots of Eranda(Ricinus communis) collected during Pravrut Ritu (EMP), Greeshma Ritu (EMG) and Shishira Ritu (EMS) shade dried separately, powdered. Spermatogenic activity study conducted on healthy albino rats divided among five groups. Testosterone was used as standard drug, whereas other three groups received sample collected in three different seasons for a period of 60 days. Next sperm analysis and histopathological study of prostate and seminal vesicle was conducted. Discussion and conclusion: Erandamoola(roots of Ricinus communis) has shown best spermatogenesis activity in experimental animals proving our ancient quotation as Vrishya. Also roots collected in different seasons have shown their difference among activity. Histopathological study of genital organs also shown positive result among spermatogenic activity.
Key words: Dravya sangrahana, Eranda(Ricinus communis), Vrishya, spermatogenesis activit
Direct nose-to-brain delivery of diazepam via trigeminal nerve contributes to rapid seizure suppression in pentylenetetrazole-induced status epilepticus model rats
Get PDFThe purpose of our present study was to elucidate the involvement of the direct transfer to the brain after intranasal (i.n.) administration of diazepam (DZP), and to provide findings whether i.n. the administration could be used to obtain rapid onset of pharmacological action. We determined the blood and brain kinetics of DZP after administrations of i.n. and other routes, and the relationship between their concentrations and rapid seizure suppression effect; furthermore, and evaluated the distribution process of DZP to the brain. There was a negative connection between the plasma concentration and the amount of DZP delivery to the brain from the systemic circulation during the period that followed intravenous and intrarectal injection before the onset of seizure suppression. I.n. administration resulted in the seizure suppression time below the correlation curve: the seizure suppression effects were observed earlier than estimated despite the low plasma concentrations of DZP, suggesting the involvement of direct nose-to-brain delivery of DZP. The time to maximum concentration (Tmax) in the forebrain, hindbrain, olfactory bulb (OB), trigeminal nerve (TN), and cerebrospinal fluid (CSF) after i.n. the administration was 3 min, which was shorter than the Tmax of the plasma concentration. In fluorescence imaging using Rhodamin-B-base, the TN and the area of the vicinity of the thalamus had stronger fluorescence 1 and 3 min after i.n. administration, compared with the OB and CSF. In summary, direct brain delivery of DZP requires the TN and it was suggested that distribution to the vicinity of the thalamus via the TN may be connected to the quick seizure suppression effect.
Keywords: Status Epilepticus, Diazepam, Intranasal Administration, Nose-to-Brain, Trigeminal Nerv
Comparative evaluation of the antioxidant and anti-inflammatory properties of Musa cavendish and Musa paradisiaca pulp and peel extracts from Guinea
Get PDFBanana is one of the most consumed fruits in the world. Musa cavendish and Musa paradisiaca cultivars differential nutrition-health properties and more specifically their antioxidant and anti-inflammatory potential are poorly known. The objective of the present study was to compare the hydroalcoholic dry extracts nutrition-health properties of these two types of Guinea bananas. Total polyphenols contents were evaluated by Folin Ciocalteu method, antioxidant capacity by DPPH, ORAC and Mito-tracker assays. Anti-inflammatory activity was evaluated in vitro on inflammatory macrophages. NO scavenging, NO and cytokines production (TNF-α and IL-6) were assessed. At 1 mg/mL, the extracts showed moderate total polyphenol content. Antioxidant activity potential was depended on the type of extracts. Banana pulps anti-inflammatory effects were demonstrated by the inhibition of NO cell production and NO scavenging suggesting that pulps have moderate anti-inflammatory effect as a function of doses (100, 50 and 25 µg/mL). However, none of the extracts inhibited the production of cytokines (TNF-α and IL-6). The present study indicates that Guinea bananas may be considered as an interesting food source of antioxidants associated to a moderate anti-inflammatory potential on specific inflammation markers.
Keywords: Banana pulp; Banana peel; Antioxidant activity; Anti-inflammatory activity; Polyphenols
Cyperus rotundus commonly used drug in Unani medicine
Get PDFHerbal medicine is the oldest form of medicine known to mankind. Cyperus rotundus L. is the world worst weed native to India, which belongs to the family Cyperaceae. It is a smooth, erect, glabrous, grass like, fibrous rooted, perennial herb that grows up to 15–60 cm height, and reproduces widely through rhizomes and tubers. Rhizomes are dark brown and woody, while stems are trigonous, green and smooth. Chemically revealed that, its consist of alkaloids, flavonoids, glycosides, phenols, tannins, steroids, starch and many novel sesquiterpenoids. In Asian countries, the rhizomes of C. rotundus, which are used as traditional folk medicine for the treatment of various ailments like amenorrhea, loss of appetite, colic, constipation, cough, diarrhea, dysentery etc.
Keyword: Cyperus rotundus, weed, rhizomes, traditional folk medicines and Diseas
Diuretic activity assessment of an aqueous extract of Hibiscus sabdariffa (Malvaceae) leaves on Wistar rats
Get PDFHibiscus sabdariffa (Malvaceae) is a plant known as a diuretic. We undertook to evaluate the therapeutic effectiveness of this plant. Twenty Wistar rats aged between 6 and 8 weeks and weighing between 150 and 250 g were divided into five homogeneous batches of four rats. Batch 1 received only the saline overload, NaCl (50 ml/kg). Immediately after the saline overload, batches 2, 3, 4 and 5 received orally, furosemide, the standard diuretic (40 mg/kg bw), or single doses of 500, 1000 and 1500 mg/kg bw of the aqueous extract of H. sabdariffa leaves, respectively. The results showed that, 24 hours after the administrations, the urinary volumetric excretions of 123.06±11.07; 66.11± 6.19; 112.22±4.36 and 61.39±10.28% respectively. The increases in urinary volumetric excretion induced by the extract were statistically significant compared to the control rats (34.99±8.46%). The extract at a dose of 1000 mg/kg bw and furosemide showed statistically similar values of urinary volumetric excretion. This urinary excretion was accompanied by an elimination of Na+ and K+ ions similar to furosemide. The urinary measurement of creatinine and urea also revealed that the extract did not interfere with normal renal function during treatment. This study shows that the aqueous extract of H. sabdariffa leaves has diuretic and natriuretic activity similar to that of furosemide. This activity could be attributed to the presence of alkaloids, steroids and flavonoids, compounds known for their diuretic effects.
Keywords: Hibiscus sabdariffa, Furosemide, urinary excretion, diureti
Associations of Electrocardiographic Abnormalities in Stable Type 2 Diabetes Subjects: Experience from a Tertiary Health Facility in South Eastern Nigeria
Get PDFIntroduction: Cardiovascular abnormalities are prevalent in the setting of diabetes mellitus, even among stable subjects, necessitating the need for a regular cardiovascular disease screening for this group of patients. Electrocardiogram is a simple and reliable screening test for cardiovascular abnormalities that could be easily accessible even in resource poor and rural settings. This study was carried out to determine the association between cardiovascular risk factors and electrocardiographic abnormalities in stable type 2 diabetes subjects in South Eastern Nigeria.
Materials and Methods: One hundred and thirty-six stable adults with type 2 diabetes mellitus were recruited consecutively from the out-patient diabetes clinic of Nnamdi Azikiwe University Teaching Hospital in South Eastern Nigeria. They were assessed for the risk factors for cardiovascular diseases that included smoking, obesity, dyslipidaemia, poor glycaemic control, hypertension, lack of exercise, presence of chronic kidney disease and metabolic syndrome. They also had a 12 lead electrocardiogram done. Results were analyzed using SPSS version 25. P value of ˂ 0.05 was considered significant.
Result: A total of 128 subjects had complete results and were analyzed. There were 63 males and 65 females with a mean age of 58.43 ± 12.85 years and mean diabetes duration of 9.03 ± 7.36 years. A total of 45.3% of the subjects had electrocardiographic abnormalities. Hypertension was present in 54.9%, dyslipidaemia in 91.4%, central obesity in 74.3%, metabolic syndrome in 76.6% and chronic kidney disease in 57.9% of the subjects. Significant association was found between smoking and occurrence of AV block (p = 0.008), central obesity and QRS axis abnormality (p = 0.002), dyslipidaemia and ST segment abnormality (p = 0.001) and lack of exercise and ST segment abnormality (p = 0.000). No significant association was found between age, sex of the subjects, duration of DM, treatment modality for DM, level of glycaemic control, hypertension, presence of CKD and metabolic syndrome and any of the electrocardiographic abnormalities.
Conclusion: Electrocardiographic abnormalities are common in stable type 2 diabetic subjects. There was significant association between smoking habit, central obesity, dyslipidaemia, lack of exercise and ECG abnormalities that included AV block, QRS axis and ST segment abnormalities
Tasar silkworm pupal oil: An excellent source of edible oil for industrial and therapeutic applications
Get PDFPolyunsaturated fatty acids are widely recognized due to their remedial properties. In our previous studies, we reported that Tasar silkworm pupal oil (TSPO) is rich in polyunsaturated fatty acids, particularly alpha-linolenic acid (ALA). Further we also extracted ALA from TSPO and reported its significant anticancer activity. In the present study, extraction of TSPO and physico-chemical characterizations including saponification, acid, peroxide, iodine pH values, and colour determination were carried out to investigate the edible properties of TSPO for commercialization as a therapeutically active functional food. Further, the anti-diabetic activity of TSPO were analyzed by α-amylase inhibition assay. The saponification (154.75 ± 0.581mg KOH/g), acid (6.24 ± 0.421 mg KOH/g), peroxide (16.20 ± 0.265 meq/kg), iodine (40.33 ± 0.577g/100 ml), pH (6.17), and colour (14 Y+1.2 R) values were within the permissible range for commercialization. In addition to this, the results of the α-amylase inhibition assay showed that TSPO exhibited an IC50 value of 207339 µg/ml. The results may facilitate the use of TSPO oil in therapeutic and functional food applications
Keywords: Characterization; Commercialization; Tasar pupal oil; Silkworm pupae