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1.
J Dent Anesth Pain Med ; 23(6): 327-335, 2023 Dec.
Article in English | MEDLINE | ID: mdl-38076501

ABSTRACT

Background: Pain control is a crucial aspect of pediatric dentistry for patient management. Thermo-mechanical devices (Buzzy™ Pain Care Labs, USA) work on the concept of vibration and cooling and have shown promising results in pain control during local anesthesia in pediatric dentistry. On the other hand, audio distraction has also been used for pain management. The amount of pain endured is determined by the patient's perception and attentiveness. Thus, if audio function is added to the thermomechanical device it might increase its efficiency. Hence, the present study aimed to compare pain on injection using a thermo-mechanical device with and without audio during inferior alveolar nerve block (IANB) injection in children aged 5-10 years old. Methods: Twenty-eight children aged between 5 and 10 indicated for IANB were included in this randomized study. Children who were undergoing the dental procedure were divided into 2 groups, with 14 children in each group. The study group was the thermo-mechanical device with audio distraction; the control group was the thermo-mechanical device without audio distraction. IANB was administered. Subjective pain evaluation was performed using the Wong-Baker Faces Pain Rating Scale (WBFPR) and objective pain evaluation was done using the Faces, Leg, Activity, Consolability, Cry (FLACC) scale. Results: The outcome depicted a significant reduction in pain on injection for both objective and subjective evaluations in the thermo-mechanical device with an audio distraction group. Conclusions: Less pain on injection was observed, when a thermo-mechanical device was used with audio distraction for IANB procedures.

3.
Drug Dev Ind Pharm ; 43(7): 1143-1153, 2017 Jul.
Article in English | MEDLINE | ID: mdl-28277848

ABSTRACT

This study was oriented toward the disintegration profiling of the diclofenac sodium (DS) immediate-release (IR) tablets and development of its relationship with medium permeability kperm based on Kozeny-Carman equation. Batches (L1-L9) of DS IR tablets with different porosities and specific surface area were prepared at different compression forces and evaluated for porosity, in vitro dissolution and particle-size analysis of the disintegrated mass. The kperm was calculated from porosities and specific surface area, and disintegration profiles were predicted from the dissolution profiles of IR tablets by stripping/residual method. The disintegration profiles were subjected to exponential regression to find out the respective disintegration equations and rate constants kd. Batches L1 and L2 showed the fastest disintegration rates as evident from their bi-exponential equations while the rest of the batches L3-L9 exhibited the first order or mono-exponential disintegration kinetics. The 95% confidence interval (CI95%) revealed significant differences between kd values of different batches except L4 and L6. Similar results were also spotted for dissolution profiles of IR tablets by similarity (f2) test. The final relationship between kd and kperm was found to be hyperbolic, signifying the initial effect of kperm on the disintegration rate. The results showed that disintegration profiling is possible because a relationship exists between kd and kperm. The later being relatable with porosity and specific surface area can be determined by nondestructive tests.


Subject(s)
Excipients/chemistry , Permeability , Tablets , Chemistry, Pharmaceutical , Kinetics , Porosity , Solubility
4.
Anticancer Agents Med Chem ; 16(11): 1355-1377, 2016.
Article in English | MEDLINE | ID: mdl-27141881

ABSTRACT

New polymer therapeutics like polymer-drug conjugates (PDCs) are developing day by day. Heterocyclic drugs with excellent cytotoxic properties are available, but lack of their specificity makes them available to the normal cells also, which is the main cause of their toxicity. Drugs in the form of PDCs make delivery possible to the specific sites. Most of the PDCs are designed with the aim to either target and/or to get activated in specific cancer microenvironments. Therefore, the most exploited targets for cancer drug delivery are; cancer cell enzymes, heat shock protein 90 (HSP90), multi-drug resistance (MDR) proteins, angiogenesis, apoptosis and cell membrane receptors (e.g., folates, transferrin, etc.). In this review, we will summarize PDCs of heterocyclic drugs, like doxorubicin (DOX), daunorubicin, paclitaxel (PTX), docetaxel (DTX), cisplatin, camptothecin (CPT), geldanamycin (GDM), etc., and some of their analogs for efficient delivery of drugs to cancer cells.


Subject(s)
Antineoplastic Agents/administration & dosage , Drug Delivery Systems , Heterocyclic Compounds/administration & dosage , Heterocyclic Compounds/chemistry , Neoplasms/drug therapy , Polymers/administration & dosage , Polymers/chemistry , Animals , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Humans , Neoplasms/pathology
6.
Appl Microbiol Biotechnol ; 67(5): 648-53, 2005 Jun.
Article in English | MEDLINE | ID: mdl-15711795

ABSTRACT

Lipase from Burkholderia multivorans was purified with high yields directly from fermentation broth by a single-step purification protocol involving adsorption and desorption. The crude enzyme (lyophilized powder) from B. multivorans was loaded on Accurel (Membrana, Germany), a polypropylene matrix, using butanol as the solvent in a buffer at pH 9.0 and ambient temperature for a period of 12 h. The enzyme adsorbed onto the matrix with high specific activity (33 units mg(-1) protein). This was followed by desorption of the enzyme from the matrix using Triton X-100 as the eluent. The enzyme was finally recovered by precipitation with acetone (50%, v/v). Thus, an overall enzyme yield of 66% with a 3.0-fold purification was obtained. The purity of the enzyme was ascertained by SDS-PAGE. The phenomenon of adsorption and desorption on Accurel was studied for three more lipases, viz. Mucor meihei lipase (Sigma-Aldrich Co.), Lipolase (Novo Nordisk, Denmark) and Pseudomonas aeruginosa lipase (laboratory isolate).


Subject(s)
Burkholderia/enzymology , Lipase/isolation & purification , Polypropylenes , 1-Butanol , Acetone , Adsorption , Electrophoresis, Polyacrylamide Gel , Fractional Precipitation , Hydrogen-Ion Concentration , Mucor/enzymology , Octoxynol , Pseudomonas/enzymology , Time Factors
7.
Crit Rev Food Sci Nutr ; 43(6): 635-44, 2003.
Article in English | MEDLINE | ID: mdl-14669881

ABSTRACT

In the present scenario, fats and oil modification is one of the prime areas in food processing industry that demands novel economic and green technologies. In this respect, tailored vegetable oils with nutritionally important structured triacylglycerols and altered physicochemical properties have a big potential in the future market. In this context, it is well established that lipases especially microbial lipases, which are regiospecific and fatty acid specific, are of immense importance and hence could be exploited for retailoring of vegetable oils. Further, of the bulk available, cheap oils could also be upgraded to synthesize nutritionally important structured triacylglycerols like cocoa butter substitutes, low calorie triacylglycerols, PUFA-enriched and oleic acid enriched oils. It is also possible to change the physical properties of natural oils to convert them into margarines and hard butter with higher melting points or into special low calorie spreads with short or medium chain fatty acids. Today, by and large, fat and oil modifications are carried out chemically following the method of directed inter-esterification. The process is energy intensive and non-specific. Lipase mediated modifications are likely to occupy a prominent place in oil industry for tailoring structured lipids since enzymatic modifications are specific and can be carried out at moderate reaction conditions. However, as a commercial venture, lipases are yet to be fully exploited. Once the technologies are established, the demand of lipases in oil industry is expected to increase tremendously in the near future for specific modifications of fats and oils to meet the changing consumers' dietary requirements.


Subject(s)
Dietary Fats, Unsaturated/metabolism , Dietary Fats/metabolism , Lipase/metabolism , Animals , Bacteria/enzymology , Esterification , Fatty Acids, Unsaturated/metabolism , Food Handling/methods , Fungi/enzymology , Humans , Lipid Metabolism , Milk, Human/chemistry , Plant Oils/metabolism , Substrate Specificity , Triglycerides/metabolism
8.
Biotechnol Appl Biochem ; 37(Pt 1): 63-71, 2003 Feb.
Article in English | MEDLINE | ID: mdl-12578553

ABSTRACT

Lipases are versatile biocatalysts that can perform innumerable different reactions. Their enantio-, chemo- and stereo-selective nature makes them an important tool in the area of organic synthesis. Unlike other hydrolases that work in aqueous phase, lipases are unique as they act at the oil/water interface. Besides being lipolytic, lipases also possess esterolytic activity and thus have a wide substrate range. Hence, the lipase assay protocols hold a significant position in the field of lipase research. Lipase activity can be estimated using a wide range of assay protocols that differ in terms of their basic principle, substrate selectivity, sensitivity and applicability. As the value of these enzymes continues to grow and new markets are exploited, development of new or improved enzymes will be a key element in the emerging realm of biotechnology. Hence, development of faster and simpler protocols incorporating newer and more specific substrates is the need of the hour. In this endeavour, methods that could be adopted for molecular screening occupy an important position. Here, an overview of the lipase assay protocols is presented with emphasis on the assays that can be adopted for the molecular screening of these biocatalysts.


Subject(s)
Lipase/chemistry , Lipase/metabolism , Enzyme Activation , Lipase/analysis , Lipase/classification , Stereoisomerism , Substrate Specificity
10.
J Biochem Biophys Methods ; 51(2): 115-20, 2002 Apr 18.
Article in English | MEDLINE | ID: mdl-12062110

ABSTRACT

A rapid screening procedure for characterization of lipase selectivities using microwaves was developed. The rate of reaction of various commercial lipases (porcine pancreas, Mucor miehei, Candida rugosa, Pseudomonas cepacia) as well as lipases from laboratory isolates-Bacillus stearothermophilus and Burkholderia cepacia RGP-10 for triolein hydrolysis was 7- to 12-fold higher in a microwave oven as compared to that by pH stat. The esterification of sucrose/methanol and ascorbic acid with different fatty acids was also achieved within 30 s in a microwave using porcine pancreas, B. stearothermophilus SB-1 and B. cepacia RGP-10 lipases. The relative rates and selectivity of the lipases both for hydrolytic and synthesis reactions remains unaltered. However, the rate of reaction was dynamically enhanced when exposed to microwaves. Microwave-assisted enzyme catalysis can become an attractive procedure for rapid characterization of large number of enzyme samples and substrates, which otherwise is a cumbersome and time-consuming exercise.


Subject(s)
Bacteria/enzymology , Biochemistry/methods , Lipase/chemistry , Microwaves , Animals , Ascorbic Acid/chemistry , Hydrogen-Ion Concentration , Hydrolysis , Lipase/metabolism , Substrate Specificity , Sucrose/chemistry , Swine , Time Factors , Triglycerides/chemistry
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