N.V. Satheesh Madhav

Bilayered Nail Lacquer of Terbinafine Hydrochloride for Treatment of Onychomycosis

The present study aimed to develop bilayered nail lacquer of terbinafine hydrochloride (TH) for treatment of onychomycosis. The composite nail lacquer formed an underlying drug-loaded hydrophilic layer and overlying hydrophobic vinyl layer. The hydrophilic lacquer made of hydroxylpropyl methylcellulose E-15 contained polyethylene glycol 400 (PEG 400) as a drug permeation enhancer. The vinyl lacquer was composed of poly (4-vinyl phenol) as a water-resistant film former. In vitro permeation studies in Franz diffusion cells indicated that the amount of TH permeated across the human cadaver nail in 6 days was 0.32 +/- 0.14, 1.12 +/- 0.42, and 1.42 +/- 0.53 microg/cm(2) from control (hydrophilic lacquer devoid of PEG 400), monolayer (hydrophilic lacquer alone), and bilayered nail lacquers, respectively. A higher nail drug load was seen in vitro with the bilayered lacquer (0.59 +/- 0.13 microg/mg) as compared to monolayer (0.36 +/- 0.09 microg/mg) and control (0.28 +/- 0.07 microg/mg) lacquers. The drug loss despite multiple washing was significantly low (p < 0.001) for the bilayered lacquer owing to the protective vinyl coating. Clinical studies demonstrated the efficacy of bilayered lacquer to achieve better drug load in the nail plate (1.27 +/- 0.184 microg/mg) compared to monolayer (0.67 +/- 0.18 microg/mg) and control (0.21 +/- 0.04 microg/mg) lacquers.

Development and evaluation of Bio-Flexy films using a novel biopolymer from Ananas cosmosus loaded with nanosized tiagabine

Background Tiagabine, an anticonvulsant drug, has t1/2: 7–9 h (low); protein binding: 96%; water solubility: 22 mg/l; it also acts as a selective GABA reuptake inhibitor. Side effects include abdominal pain, pharyngitis, suicidal thoughts, and sudden unexpected death. Aim The aim of this work was to formulate nanosized Bio-Flexy films using a novel biopolymer isolated from Ananas cosmosus fruit pulp containing tiagabine as a model drug. The soft palate drug delivery helps bypass first-pass metabolism in the liver and presystemic elimination in the gastrointestinal tract is avoided. The biopolymer isolated from A. cosmosus was used to prepare Bio-Flexy films because of its biodegradability and biocompatibility, and because it is nontoxic and nonirritant, and nonreactive on soft palatal surfaces. Physicochemical characterization of the biopolymer showed its inbuilt property as film forming ability and mucoadhesivity which was confirmed, screened and authenticated. Materials and methods Bio-Flexy films were prepared using the solvent casting technique. The drug to polymer ratio was chosen at five levels for A. cosmosus FPA1–FPA5 with varying ratios of biopolymer from 1 to 10 and 1% of nanosized tiagabine and compared with sodium carboxyl methyl cellulose standard films. Bio-Flexy films were evaluated for thickness, surface pH, weight uniformity, folding endurance, in-vitro release, and stability studies. Results The percentage yield of the A. cosmosus biopolymer was found to be 0.972±0.008%. The thickness of the formulated Bio-Flexy films ranged from 0.041 to 0.091 mm, the folding endurance was 65–95, the surface pH was 7.01±0.02 to 7.01±0.01, and weight uniformity was 0.001±0.02 to 0.032±0.01. Conclusion On the basis of all the above-mentioned evaluation parameters, formulation FPA3 [containing Tiagabine: Ananas cosmosus biopolymer (1:5)] was selected as the best film as results of an in-vitro release study showed prolonged durationof 48 h in prolonged manner. The best film showed R2=0.969 release pattern by Peppas–Korsmeyer, as the Best Fit model, followed by anomalous transport release mechanism, which was confirmed by using BITS Software 1.12. Stability study showed stable Bio-Flexy films with no significant change in physical appearance and stable pH. Prepared formulations of tiagabine-loaded Bio-Flexy films are suitable for soft palatal delivery.

Development and evaluation of nanosized aripiprazole-loaded bioflexy films using a biopolymer from Lagenaria siceraria for brain delivery through orosoft palatal mucosal platform

Purpose The National Institute of Mental Health estimated the global cost of mental illness to be

Formulation and in-vitro preliminary screening of polyphyto antilithiatic combination

6T by 2030. The purpose of the study was to deliver aripiprazole for brain targeting by suitably designing a bioflexy film for the treatment of different brain disorders. Materials and methods Bioflexy films were prepared by solvent casting technique using aripiprazole as a model drug, different concentrations of isolated biopolymer from Lagenaria siceraria, and a standard polymer. Results All formulations of aripiprazole were flexible, smooth, and transparent in nature, with a weight range from 23.73 to 34.48 mg, pH range from 7.27 to 7.39, and folding endurance of 94–116 times. The content uniformity was in the range of 97.2–98.6. Conclusion In-vitro and in-vivo release shows FL2 as the best formulation. On the basis in-vitro and in-vivo drug release, FL2 was found to be best formulation showing mucoadhesivity (36 h), t50% of 2.5 h, t80% of 23.4 h, and having R2 value of 0.9923, best-fit model Higuchi matrix analyzed by BIT-SOFT 1.12. Moreover, it was observed that significant amount of drug reaches to the brain through soft palatal route through neural pathway.

DEVELOPMENT AND EVALUATION OF NOVEL REPAGLINIDE BIO STRIPS FOR TRANSLAB IAL DELIVERY

Abstract Objective To study people suffered from urinary stone problem by calcium oxalate monohydrate (COM) and calcium oxalate dihydrate (COD) containing stones. Methods In the present study, CO crystals were grown by mixing and stirring two equal volumes of solutions A and B. Two solutions of following composition were mixed: A: Na2C2O4(2 mmol) and B: CaCl2·2H2O (10 mmol). The crystals after incubation in tris buffer were then subjected to the aqueous extract of the polyherbal formulation and cystone was taken as standard. Results After the treatment with the extract the crystals were microscopically examined and elemental analysis for calcium was carried out. The formulation proved out to be very effective against the CO crystals. Conclusions The results have come out to be very motivating and further pharmacological study could be carried out on the samples to reveal an effective drug for the urolithiasis. Data reveals that phytotherapeutic agents could be useful as either an alternative or a complementary therapy in the management of urolithiasis.

A novel smart mucoadhesive biomaterial from Lallimantia royalena seed coat

The aim of this study was to explore the potentiality of lip skin as a novelistic Translabial drug delivery platform due to i ts unique histology and by formulating drug loaded bio lip strips using novel bio - excipients which was isolated from the seeds of z ea mays by simplified economical process and purified by hot dialysis method. Repaglinide loaded bio - lip strips were formulated by using zea mays bio - material as a strip former and dextrose as a flexicizer. The formulated strips were subjected for various evaluation parameters like thickness, folding endurance and in - vitro and In - vivo drug release. Present study revealed that the biopolymer possessing promising strip ability . The Repaglinide release was extended over a period of 24 hrs and by fitting the dr ug release data into zero order, first order and Higuchi model, it was concluded that drug release from strips followed Higuchi model an d the mechanism of the drug release was diffusion and anomalous type. On the basis of above parameters and used concen tration of biopolymer in the formulation, F2 was selected as the best formulation. The in vitro and in - vivo studies have shown the potential of the Repaglinide loaded bio strip for sustained delivery through Translabial route.