Thyme Oil-Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery.

The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (23 factorial design-based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 23 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting for optimized formulation (FO) was A= 4.96, B= 3.82, and C= 2.16. The optimized transferosomes showed 52.38 ± 1.76% DEE, 76.37 nm vesicle size, 0.233 PDI, - 20.3 mV zeta potential, and desirable deformability. TEM of optimized transferosomes exhibited a multilamelar structure. FO bigel's FE-SEM revealed a globule-shaped vesicular structure. Further, the optimized transferosomal suspension was incorporated into thyme oil (0.1% w/w)-containing bigel (TO-FO). Ex vivo transdermal fluconazole permeation from different transferosomal bigels was sustained over 24 h. The highest permeation flux (4.101 µg/cm2/h) was estimated for TO-FO bigel. TO-FO bigel presented 1.67-fold more increments of antifungal activity against Candida albicans than FO bigel. The prepared thyme oil (0.1% w/w)-containing transfersomal bigel formulations can be used as topical delivery system to treat candida related fungal infections.

Chitosan-carboxymethyl tamarind gum in situ polyelectrolyte complex-based floating capsules of ofloxacin: In vitro-in vivo studies.

The current research attempted to design and evaluate sustained stomach-specific ofloxacin delivery by single-unit hydrodynamically balanced system (HBS)-based floating capsules. These HBS-based floating capsules of ofloxacin were prepared using two oppositely ionic polymers, namely cationic-natured low molecular mass chitosan (LMMCH) and anionic-natured carboxymethyl tamarind gum (CMTG). FTIR results indicated the in situ formation of a polyelectrolyte complex in-between two oppositely charged polymers (i.e., in-between -NH2 group of the cationic natured LMMCH and -COOH groups of the anionic natured CMTG) and the nonexistence of any drug-polymer interaction(s) within these formulated ofloxacin HBS capsules. All these LMMCH-CMTG ofloxacin HBS capsules exhibited drug content uniformity, a sustained in vitro drug-releasing profile over 10 h. The ofloxacin HBS capsules (formulated with 75 mg LMMCH and 25 mg CMTG), which was selected as best formulation (for further studies), exhibited excellent in vitro floatation behaviour in SGF (pH 1.2) over 6 h without any floating lag-time, whereas the same formulation containing barium sulfate (100 mg) instead of drug demonstrated prolonged stomach-specific gastroretention in an in vivo X-ray imaging study using rabbits. Therefore, these types of HBS floating capsules can be useful for stomach-specific gastroretentive floating delivery of other drugs.

Improved Fault Classification in Series Compensated Transmission Line: Comparative Evaluation of Chebyshev Neural Network Training Algorithms.

This paper presents the Chebyshev neural network (ChNN) as an improved artificial intelligence technique for power system protection studies and examines the performances of two ChNN learning algorithms for fault classification of series compensated transmission line. The training algorithms are least-square Levenberg-Marquardt (LSLM) and recursive least-square algorithm with forgetting factor (RLSFF). The performances of these algorithms are assessed based on their generalization capability in relating the fault current parameters with an event of fault in the transmission line. The proposed algorithm is fast in response as it utilizes postfault samples of three phase currents measured at the relaying end corresponding to half-cycle duration only. After being trained with only a small part of the generated fault data, the algorithms have been tested over a large number of fault cases with wide variation of system and fault parameters. Based on the studies carried out in this paper, it has been found that although the RLSFF algorithm is faster for training the ChNN in the fault classification application for series compensated transmission lines, the LSLM algorithm has the best accuracy in testing. The results prove that the proposed ChNN-based method is accurate, fast, easy to design, and immune to the level of compensations. Thus, it is suitable for digital relaying applications.

Zinc alginate-carboxymethyl cashew gum microbeads for prolonged drug release: development and optimization.

Isoxsuprine HCl-loaded microbeads using sodium alginate (SA)-carboxymethyl cashew gum (CMCG) polymer-blends were developed through ionotropic-gelation technique using ZnSO4 as cross-linker. Effects of polymer-blend ratio and cross-linker concentration on drug encapsulation efficiency (DEE) and cumulative drug release at 7 h (R7 h) were optimized by 3(2) factorial design. Optimized microbeads were of excellent combination of high DEE (79.92±2.51%) and suitable sustained drug release pattern over a prolonged period of 7 h (58.67±2.26%). The microbead surface morphology was analyzed by SEM. The physical state of isoxsuprine HCl within the optimized microbead matrix was analyzed by FTIR and DSC. In vitro isoxsuprine HCl release from alginate-CMCG microbeads in phosphate buffer (pH, 6.8) showed prolonged sustained drug release and Korsmeyer-Peppas model (R2=0.9959-0.9992) over 7 h.

Topical gels of lidocaine HCl using cashew gum and Carbopol 940: preparation and in vitro skin permeation.

The present study was attempted to prepare novel topical gels of 4% lidocaine HCl using cashew gum and Carbopol 940. The prepared gels were evaluated for pH, viscosity, and in vitro skin permeation through excised porcine skin. The pH of these topical gels was found within the range of 5.98-6.06; whereas, the viscosity was found 4.58 × 10(6) to 4.88 × 10(6) cps. The in vitro skin permeation from these gels showed permeation flux range, 851.34 ± 9.16 to 1568.15 ± 14.03 µg/cm(2)/h. The highest permeation flux (1568.15 ± 14.03 µg/cm(2)/h) was observed, when 0.01% menthol was added, which was higher than that of the marketed 4% lidicaine HCl topical gel (1355.41 ± 10.92 µg/cm(2)/h). These topical gels found best-fit with Korsmeyer-Peppas model and almost the super case-II transport mechanism. The stability study revealed that these gels were physically stable without occurrence of syneresis.

Gastroretentive hydrodynamically balanced systems of ofloxacin: In vitro evaluation.

Hydrodynamically balanced systems (HBSs) of ofloxacin were prepared using lactose, HPMC K4M, PVP K 30, and liquid paraffin, which may increase the mean residence time in the gastrointestinal tract, and may be able to provide maximum drug at the site of absorption to improve oral bioavailability. All these formulated HBS capsules were floated well over 6 h with no floating lag time. They also showed sustained drug release over 6 h. Time for 50% release of ofloxacin was within the range, 2.47 ± 0.02 to 3.07 ± 0.08 h. The in vitro drug release from these HBS capsules was dependent on HPMC K4M, PVP K 30, and liquid paraffin content. The drug release pattern of these HBS capsules containing ofloxacin followed the Higuchi model with the anomalous transport mechanism.

Calcium alginate/gum Arabic beads containing glibenclamide: development and in vitro characterization.

This work investigates the development, optimization and in vitro characterization of calcium alginate/gum Arabic beads by an ionotropic gelation method for prolonged sustained release of glibenclamide. The effects of amount of sodium alginate and gum Arabic as independent process variables on the drug encapsulation efficiency and drug release were optimized and analyzed based on central composite design and response surface methodology. Increment in drug encapsulation efficiency and decrease in drug release were found with the increase of both the amounts of sodium alginate and gum Arabic, used as polymer-blend. These optimized beads showed high drug encapsulation efficiency (86.02±2.97%), and suitable sustained drug release pattern over prolonged period (cumulative drug release after 7 h of 35.68±1.38%). The average size of these formulated dried beads containing glibenclamide ranged from 1.15±0.11 to 1.55±0.19 mm. The in vitro dissolution of these beads showed prolonged sustained release of glibenclamide over 7 h, which followed first-order model (R(2)=0.9886-0.9985) with anomalous (non-Fickian) diffusion mechanism (release exponent, n=0.72-0.81). The swelling and degradation of the optimized beads were influenced by pH of test mediums. These beads were also characterized by SEM and FTIR spectroscopy for surface morphology and excipients-drug interaction analysis, respectively. These developed calcium alginate/gum Arabic beads containing glibenclamide could possibly be advantageous in terms of advanced patient compliance with reduced dosing interval.