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52. Luliconazole-loaded nanostructured lipid carriers for topical treatment of superficial Tinea infections

Author

Baghel, Saahil, Nair, Vishnumaya S., Pirani, Asma, Sravani, Anne Boyina, Bhemisetty, Brahmam, Ananthamurthy, Koteshwara, Aranjani, Jesil Mathew, Lewis, Shaila A., Baghel, Saahil, Nair, Vishnumaya S., Pirani, Asma, Sravani, Anne Boyina, Bhemisetty, Brahmam, Ananthamurthy, Koteshwara, Aranjani, Jesil Mathew, and Lewis, Shaila A.

Abstract

Tinea are superficial fungal infections caused by dermatophytes. Luliconazole exhibits highest antifungal activity against Trichophyton spp. which are major causative agents of dermatophytosis. However, luliconazole suffers from drawbacks such as less skin retention, low aqueous solubility and poor skin penetration. To overcome the limitations of luliconazole, nanostructured lipid carriers (NLCs) were formulated. NLCs are better permeation enhancers as they increase skin occlusion and hydration. The selection of various lipids and surfactants was based on the solubility of luliconazole in these components. Luliconazole NLC dispersion was prepared by hot melt emulsification technique followed by probe sonication. The dispersion was incorporated into a gel composed of Sepineo P 600 under magnetic stirring. in vitro antifungal studies were carried out with optimized luliconazole NLC gel, marketed luliconazole cream and control (luliconazole in gel base) against pathogenic Trichophyton rubrum. Ex-vivo diffusion study demonstrated that NLCs incorporated into gel exhibited greater retention on skin. In-vivo skin irritancy study showed no signs of erythema or edema post 24, 48, and 72 h at site of application. In comparison with marketed cream and based on the zone of inhibition diameters, NLC formulation was found to be very effective against Trichophyton rubrum.

Published
2020

73. Perspectives in Nanosuspension drug delivery.

Author

Sunil B., Singh, Alka K., Naik, Anantha N., Dwibhashyam, V. S. N. Murthy, and Lewis, Shaila A.

Subjects
PRECIPITATION (Chemistry), DRUG delivery systems, SUSPENSIONS (Chemistry), BIOAVAILABILITY, SOLUBILITY
Abstract

The effectiveness of many drugs is limited due to poor oral bioavailability; the chief reason for this being poor solubility in both aqueous and organic solvents. The technology of nanosuspension has become one of the promising strategies to overcome bioavailability issues associated with poorly soluble BCS Class II and Class IV molecules. The specific features of nanosuspensions have enabled their use in various dosage forms. A number of nanosuspension based drug products have successfully reached the market. This review is intended to give an overview of nanosuspension, and highlight the various formulation techniques, nanosuspension characterization, surface modification, recent technological advances and its different applications. [ABSTRACT FROM AUTHOR]

Published
2018

75. Design and evaluation of sustained-release matrix once daily formulation of stavudine

Author

Kumar, Dhirendra; Manipal College of Pharma. Sci.Manipal-576104, Karnataka, India, Dave, Vivek; Manipal College of Pharma. Sci. Manipal-576104, Karnataka, India, Lewis, Shaila; Manipal College of Pharma. Sci. Manipal-576104, Karnataka, India, Parmar, Brajesh; Dept. Of Pharm. sci. Barkatullah University, Bhopal, (MP) India, Gajbhiye, Kavita R.; Sagar Institute of Pharm. Sci., Sagar (MP) India, Paliwal, Sarvesh; Banasthali University Dept. of Pharmaceutical Chemistry Banasthali, Rajasthan, India, Kumar, Dhirendra; Manipal College of Pharma. Sci.Manipal-576104, Karnataka, India, Dave, Vivek; Manipal College of Pharma. Sci. Manipal-576104, Karnataka, India, Lewis, Shaila; Manipal College of Pharma. Sci. Manipal-576104, Karnataka, India, Parmar, Brajesh; Dept. Of Pharm. sci. Barkatullah University, Bhopal, (MP) India, Gajbhiye, Kavita R.; Sagar Institute of Pharm. Sci., Sagar (MP) India, and Paliwal, Sarvesh; Banasthali University Dept. of Pharmaceutical Chemistry Banasthali, Rajasthan, India

Abstract

The aim of the present study was to formulate once daily sustained release matrix tablets of Stavudine to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance. The sustained release tablets were prepared by direct compression and formulated using different drug: polymer ratios, formulations such as F1to F15. Hydrophilic polymers like Hydroxy propyl methyl cellulose (HPMC), Carboxymethyl cellulose (CMC) and Starch 1500 were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with pharmacopoeial standards. Formulation containing Stavudine:HPMCK15: Na-CMC (1:2:0.5) with hardness 10-11kg/cm2 showed the desired release profile which matched the theoretical release profile. SEM studies of the formulations were carried out for the confirmation of mechanism of drug release. The in vitro drug release characteristics were studied in both simulated gastric and intestinal fluids for a period of 24 hr using USP Type 2 dissolution apparatus. Mathematical analysis of the release kinetics indicated a coupling of diffusion and erosion mechanisms. The study proves that the developed sustained release tablet is capable of releasing the drug in a sustained manner for 24 hr.Keywords: Sustained release; Matrix tablets; Hydroxy propyl methylcellulose; Stavudine

Published
2011

83. Smart Drug Delivery Systems as Game Changers in Therapeutics.

Author

Bhandari, Amita, Naik, Anantha N., and Lewis, Shaila

Subjects
NOOTROPIC agents, DRUG delivery systems, DOSAGE forms of drugs, AMPHOTERICIN B, LIPOSOMES
Abstract

Smart Drug Delivery Systems (SDDS) have emerged as panacea for many clinically useful drugs weighed down with toxicity. The discovery of Amphotericin B as a liposome has raised hopes and directed mammoth efforts in SDDS. The concept of manipulation of toxicity has given rise to additional significant approaches like targeting and use of physico-chemical approaches. Currently the spectrum of SDDS comprises of targeting liposomes, drug loaded biodegradable microspheres, stimuli responsive drug polymer conjugates, smart hydrogels, polymeric micellar particles, intelligent lipoprotein carriers, and nano carriers. There is a wealth of knowledge accumulated worldwide in the area of SDDS, which can be extremely beneficial to industry as well as practitioners of health care. In this article an overview of developments are reviewed. [ABSTRACT FROM AUTHOR]

Published
2013
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84. Design and in vitro/in vivoevaluation of extended release matrix tablets of nateglinide

Author

Sharma, Pushkar R. and Lewis, Shaila A.

Abstract

Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily.

Published
2013
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85. In vitro-in silicoevaluation of Apremilast solid dispersions prepared via Corotating Twin Screw Extruder

Author

Muvva, Aneesh, Lakshman, Dani, Dwibhashyam, V.S.N. Murthy, Dengale, Swapnil, and Lewis, Shaila A.

Abstract

The purpose of this study was to employ the Hot melt extrusion technique (HME) to prepare amorphous solid dispersions (ASDs) of Apremilast, a BCS class IV drug. Drug–polymer miscibility was assessed with solubility parameter and the Flory-Huggins equation. Soluplus® was selected as the carrier and solid dispersions were prepared in 10:90, 30:70 and 50:50 drug: polymer ratios. The study evaluated the influence of drug loading and extrusion temperature on the solid dispersions. The produced solid dispersion were characterized using FTIR, DSC and XRD. Pharmacokinetics of Apremilast following oral delivery of the solid dispersion formulations were predicted in silicousing GastroPlus™. The extruder processing temperature had a profound influence on the generation of ASDs. Solid-state characterization exhibited amorphous nature of drug in the solid dispersion samples. The constructed in silicomodel predicted more than 50% of increase in Apremilast Cmax and AUC values from solid dispersion formulations compared to plain Apremilast. In conclusion, the Apremilast ASDs formulated with Soluplus® showed a significant increase in solubility and may be considered as a favorable approach for enhancing Apremilast oral bioavailability. Stress samples stored at 25 °C/75% RH condition for 10 days showed decrease in dissolution profile for ASDs with 50% and 90% Soluplus® and no change was observed in ASDs with 70% Soluplus®. Based on the conducted studies, an optimum drug: polymer ratio of 30:70 was suggested for Apremilast: Soluplus® ASDs for further development.

Published
2020
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86. Enhancement of Aqueous Solubility and Oral Bioavailability of Nelfinavir by Complexation with ß- Cyclodextrin.

Author

Kumari, Shilpi, Bhawar, Ganesh T., Musmade, Prashant B., and Lewis, Shaila

Subjects
*DRUG bioavailability, *NELFINAVIR, *SOLUBILITY product, *ORAL drug administration, *CYCLODEXTRINS, *AQUEOUS solutions
Abstract

Purpose: To determine if complexation with β- cyclodextrin (β-CD) increases water solubility and subsequent bioavailability of nelfinavir mesylate (NM). Methods: Complexation of NM with β-CD in 1:1.5 molar ratio was carried out by solvent evaporation, freeze-drying and kneading methods. The complexes were characterized by Fourier transform infrared spectroscopy (FTIR). The in vitro solubility of the pure drug as well as that of the complexes was evaluated using USP type 2 apparatus. One of the drug complexes was also evaluated in vivo using Wistar rats to determine its pharmacokinetic profile. Results: Freeze-dried NM-βCD complex was selected for in vivo studies based on its free flowing property and superior texture. The complexes prepared by the three methods all showed largely similar dissolution rate. The in vivo pharmacokinetic study of the freeze-dried complex in male Wistar rats showed significant increase in Cmax, tmax and AUC (p ≤ 0.05) compared to those of the plain drug. Conclusion: These findings suggest that complexation of NM with β-CD is an effective and promising approach to increasing the oral bioavailability of NM. [ABSTRACT FROM AUTHOR]

Published
2015
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