Institute for Drug Delivery and Biomedical Research

Bangalore, India

Institute for Drug Delivery and Biomedical Research

Bangalore, India
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Rangappa S.,University of Mississippi | Rangan K.K.,Materials Modification, Inc. | Sudarshan T.S.,Materials Modification, Inc. | Narasimha Murthy S.,University of Mississippi | Narasimha Murthy S.,Institute for Drug Delivery and Biomedical Research
Journal of Drug Delivery Science and Technology | Year: 2017

The objective was to evaluate anti-nociceptive activity of a novel clay based dermal patch system for potential use in first degree burn wounds. First, clay patches with silver were formulated for antisepsis. Subsequently they were loaded with 5 mg/cm2 of lidocaine. The skin penetration studies were performed to ensure the delivery of drug into the skin. Finally, the lidocaine loaded silver clay patches were screened for in-vivo anti-nociception using hot plate analgesiometer in rats. The lidocaine loaded silver clay patches did not show anti-nociception after 6hrs of application despite significant amount of drug release observed in in-vitro studies. To discover the reason for failure of the patch system in thermally induced pain model, mechanistic studies were performed using clay patches not loaded with silver colloid. When lidocaine loaded clay patches, devoid of silver were subjected to in-vivo evaluation, a significant anti-nociceptive activity was observed. The reason for masking of anti-nociceptive activity of lidocaine in the silver loaded patches was potentially due to coating of silver on the paw rendering the skin more conductive. Often, additional mechanistic studies are required to be performed to critically assess the in-vivo data. © 2017 Elsevier B.V.


Angamuthu M.,University of Mississippi | Nanjappa S.H.,Institute for Drug Delivery and Biomedical Research | Raman V.,University of Mississippi | Jo S.,University of Mississippi | And 3 more authors.
Journal of Pharmaceutical Sciences | Year: 2014

Controlled-release drug delivery systems based on biodegradable polymers have been extensively evaluated for use in localized drug delivery. In the present study, intralesionally injectable poly (lactide-co-glycolide) (PLGA) microspheres for controlled release of terbinafine hydrochloride (TH) was developed for treating fungal toe/finger nail infections. TH-PLGA microspheres were formulated using O/W emulsification and modified solvent extraction/evaporation technique. Microspheres were evaluated for particle size and size distribution, encapsulation efficiency, surface, and morphology. The in vitro drug release profile was studied in aqueous media as well as in 1% agar gel. Microspheres system was also evaluated in excised cadaver toe model, and extent of TH accumulation in nail bed, nail plate, and nail matrix was measured at different time points. Microspheres were found to provide consistent and sustained TH release. Intralesional administration of controlled-release microspheres can be a potential alternative mode of treating fungus-infected toe and/or finger nails. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.


Kushwaha A.S.,University of Mississippi | Sharma P.,University of Mississippi | Shivakumar H.N.,Institute for Drug Delivery and Biomedical Research | Rappleye C.,Ohio State University | And 3 more authors.
AAPS PharmSciTech | Year: 2017

AR-12 is a novel small molecule with broad spectrum antifungal activity. Recently, AR-12 was found to be highly active against Trichophyton rubrum, one of the predominantly responsible organisms that cause onychomycosis. The primary objective of this project was to investigate the ability of AR-12 to penetrate into and across the human nail plate followed by improving its trans-ungual permeation using different penetration enhancers. TranScreen-N™, a high throughput screening method was utilized to explore the potential nail penetration enhancers to facilitate the drug delivery through the nail. This screen demonstrated that dexpanthenol and PEG 400 were the most efficient enhancers. The in vitro permeation studies were performed across the human cadaver nail plates for 7 days with three AR-12 (5% w/v) formulations containing 10% w/v dexpanthenol (Formulation A), 10% w/v PEG 400 (Formulation B), and a combination of 10% w/v dexpanthenol + 10% w/v PEG 400 (Formulation C). The in vitro studies concluded that dexpanthenol and PEG 400 were able to deliver a significant amount of AR-12 into and across the nail plate that was found to be more than MIC 50 level of the drug. © 2017 American Association of Pharmaceutical Scientists


Manda P.,University of Mississippi | Kushwaha A.S.,University of Mississippi | Kundu S.,Mississippi State University | Shivakumar H.N.,Institute for Drug Delivery and Biomedical Research | And 4 more authors.
Journal of Controlled Release | Year: 2016

The purpose of the current study was to investigate the plausibility of delivery of ziconotide to the cerebrospinal fluid (CSF) via intranasal administration. Ziconotide was administered either in the form of solution or Kolliphor P 407 gels (KP 407) intranasally in Sprague-Dawley rats. The effect of incorporation of chitosan in the formulation was also investigated. Time course of drug in the CSF was investigated by collecting CSF from cisterna magna. Pharmacokinetics of ziconotide in CSF following intrathecal and intravenous (i.v.) administration of ziconotide was investigated. Upon intrathecal administration the elimination rate constant of ziconotide in CSF was found to be 1.01 ± 0.34 h- 1. The Cmax and Tmax of ziconotide in CSF following intravenous administration were found to be 37.78 ± 6.8 ng/mL and ~ 2 h respectively. The time required to attain maximum concentration (Tmax) in CSF was less upon intranasal administration (15 min) compared to i.v. administration (120 min). Presence of chitosan enhanced the overall bioavailability of ziconotide from intranasal solution and gel formulations. The elimination rate constant of ziconotide in CSF following intranasal and intravenous administration of ziconotide solution was found to be 0.54 ± 0.08 h- 1 and 0.42 ± 0.10 h- 1 respectively. Whereas, intranasal administration of ziconotide in the form of in situ forming gel lowered the elimination rate significantly. These results suggest that intranasal administration could be a potential noninvasive and patient compliant method of delivering ziconotide to CSF to treat chronic pain. © 2015 Elsevier B.V.


Juluri A.,University of Mississippi | Popescu C.,Roquette America Inc | Zhou L.,Roquette America Inc | Murthy R.N.,Institute for Drug Delivery and Biomedical Research | And 6 more authors.
AAPS PharmSciTech | Year: 2016

The objective of this project was to investigate the potential of Kleptose Linecaps DE17 (KLD) in masking the unpleasant/bitter taste of therapeutic agents by hot melt extrusion (HME). Griseofulvin (GRI) and caffeine anhydrous (CA) were used as a bitter active pharmaceutical ingredient (API) model drugs. Thermogravimetric studies confirmed the stability of GRI, CA, and KLD at the employed extrusion temperatures. The differential scanning calorimetry (DSC) studies revealed a characteristic melting endotherm of GRI at 218–220°C and CA at 230–232°C in the physical mixtures as well as in all extrudates over the period of study, indicating the crystalline nature of drug. HME of KLD was achieved only in the presence of plasticizer. Among the several plasticizers investigated, xylitol showed improved processability of KLD at 15% w/w concentration. Dissolution studies of HME extrudates using simulated salivary medium exhibited ∼threefold less release compared to physical mixture at the end of 5 min (the lesser drug release, better the taste masking efficiency). Furthermore, the results from the sensory evaluation of products in human panel demonstrated strong bitter taste in the case of physical mixture compared to the HME formulation, suggesting the potential of Kleptose Linecaps DE17 as taste masking polymer in melt extruded form. © 2015, American Association of Pharmaceutical Scientists.


Manda P.,University of Mississippi | Angamuthu M.,University of Mississippi | Hiremath S.R.,Institute for Drug Delivery and Biomedical Research | Raman V.,University of Mississippi | And 2 more authors.
Journal of Pharmaceutical Sciences | Year: 2014

Topical treatment of hypertrophic scars is challenging because of poor penetrability of drugs into the scar tissue. The objective of the study was to investigate the effectiveness of iontophoresis to deliver medicaments across the scar epidermis. Initially, biophysical studies were performed to investigate the differences between scar and normal skin epidermis obtained from cadaver. In case of scar skin epidermis, the transepidermal water loss was not significantly different from the normal skin epidermis, whereas the electrical resistivity was significantly higher. The passive permeation flux of sodium fluorescein was approximately one-third of that across the normal skin epidermis. Scanning electron microscopy studies revealed that the two membranes were alike except that the scar skin epidermis lacked follicles. Cathodal iontophoresis enhanced the delivery of sodium fluorescein across the scar skin epidermis by approximately 46 folds [51.90 ± 8.82 ng/(cm2 h)]. However, the transport of sodium fluorescein across the scar skin epidermis was about an order of magnitude less than the normal skin epidermis. Overall, the studies suggest that iontophoresis could be utilized to overcome the barrier resistance of scar skin epidermis and treat the scar regionally. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.


PubMed | Institute for Drug Delivery and Biomedical Research, Visveswarapuram Institute of Pharmaceutical science, University of Mississippi and Roquette America Inc.
Type: Journal Article | Journal: AAPS PharmSciTech | Year: 2016

The objective of this project was to investigate the potential of Kleptose Linecaps DE17 (KLD) in masking the unpleasant/bitter taste of therapeutic agents by hot melt extrusion (HME). Griseofulvin (GRI) and caffeine anhydrous (CA) were used as a bitter active pharmaceutical ingredient (API) model drugs. Thermogravimetric studies confirmed the stability of GRI, CA, and KLD at the employed extrusion temperatures. The differential scanning calorimetry (DSC) studies revealed a characteristic melting endotherm of GRI at 218-220C and CA at 230-232C in the physical mixtures as well as in all extrudates over the period of study, indicating the crystalline nature of drug. HME of KLD was achieved only in the presence of plasticizer. Among the several plasticizers investigated, xylitol showed improved processability of KLD at 15% w/w concentration. Dissolution studies of HME extrudates using simulated salivary medium exhibited threefold less release compared to physical mixture at the end of 5min (the lesser drug release, better the taste masking efficiency). Furthermore, the results from the sensory evaluation of products in human panel demonstrated strong bitter taste in the case of physical mixture compared to the HME formulation, suggesting the potential of Kleptose Linecaps DE17 as taste masking polymer in melt extruded form.


PubMed | University of Seoul, Institute for Drug Delivery and Biomedical Research, University of Mississippi, Ashland Specialty Ingredients and Visveswarapuram Institute of Pharmaceutical science
Type: Journal Article | Journal: International journal of pharmaceutics | Year: 2015

The objective of this study was to develop caffeine citrate orally disintegrating tablet (ODT) formulations utilizing hot-melt extrusion technology and evaluate the ability of the formulation composition to mask the unpleasant bitter taste of the drug using in vitro and in vivo methods. Ethylcellulose, along with a suitable plasticizer, was used as a polymeric carrier. Pore forming agents were incorporated into the extruded matrix to enhance drug release. A modified screw configuration was applied to improve the extrusion processability and to preserve the crystallinity of the API. The milled extrudates were subjected to dissolution testing in an artificial salivary fluid and investigations using e-tongue, to assess the extent of masking of bitter taste of the API. There was an insignificant amount of drug released from the formulation in the salivary medium while over 80% of drug released within 30 min in 0.1N HCl. ODTs were also developed with the extrudate mixed with mannitol and crospovidone. The quality properties such as friability and disintegration time of the ODTs met the USP specifications. The lead extrudate formulations and the ODTs prepared using this formulation were subjected to human gustatory evaluation. The formulations were found to mask the unpleasant taste of caffeine citrate significantly.


Kushwaha A.,University of Mississippi | Shivakumar H.N.,Institute for Drug Delivery and Biomedical Research | Murthy S.N.,Bangalore University
Drug Development and Industrial Pharmacy | Year: 2016

In present studies, a hyponychium pathway (from ventral side of the nail plate) was investigated as a potential route of drug delivery into the nail apparatus using iontophoresis as an active physical method. In vitro transport studies were performed across the human nail plate using sodium fluorescein as a marker substrate for 24 h. After transport studies, the amount of sodium fluorescein extracted from an active diffusion area of the nail plate in case of iontophoresis was found to be ∼54-folds more to that of passive. The amount of sodium fluorescein retained in the peripheral area of the nail plate after application of iontophoresis was found to be ∼30-folds more relative to passive. Ex vivo transport studies were performed on excised human cadaver toe using terbinafine hydrochloride as a model drug for three days (8 h/day). The amount of terbinafine retained in the nail plate after application of iontophoresis (3.43 ± 1.34 µg/mg) was ∼20-folds more when compared with passive (0.17 ± 0.10 µg/mg). The amount of drug extracted from the nail bed and nail matrix was 1.73 ± 0.12 µg/mg and 0.55 ± 0.22 µg/mg, respectively. On the other hand, there was no detectable amount of terbinafine found in the nail bed and nail matrix in case of control (passive delivery). These studies show that the iontophoretic drug delivery through hyponychium region to other parts of the nail apparatus could be a potential way of onychomycosis treatment. © 2016 Informa UK Limited, trading as Taylor & Francis Group


Maurya A.,University of Mississippi | Narasimha Murthy S.,University of Mississippi | Narasimha Murthy S.,Institute for Drug Delivery and Biomedical Research
Journal of Pharmaceutical Sciences | Year: 2014

The use of chemical penetration enhancers (CPEs) is one of the most common approaches to improve the dermal and transdermal delivery of drugs. However, often, incorporation of CPEs in the formulation poses compatibility and stability challenges. Moreover, incorporation of enhancers in the formulation leads to prolonged exposure to skin increasing the concern of causing skin reactions. This study was undertaken to assess whether pretreatment with CPEs is a rational approach to enhance the permeation of diclofenac sodium. In vitro experiments were performed across porcine epidermis pretreated with propylene glycol or oleic acid or their combinations for 0.5, 2, and 4 h, respectively. Pretreatment with combination of oleic acid in propylene glycol was found to enhance the permeation of diclofenac sodium significantly only at 10% and 20% (v/v) level, and only when the pretreatment duration was 0.5 h. Longer durations of pretreatment and higher concentration of oleic acid in propylene glycol did not enhance the permeation of diclofenac sodium. In vivo dermatokinetic studies were carried out on Sprague-Dawley rats. A twofold increase in AUC and C max was observed in case of rats pretreated with enhancers over the group that was pretreated with buffer. In conclusion, this study showed that composition of the enhancers and duration of pretreatment are crucial in determining the efficacy of CPEs. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.

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