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The present study aimed to enhance the transdermal delivery of lacidipine by niosomal vesicles. Lacidipine niosomes were generated using the ultrasonic method, and Span 60 was used as a nonionic surfactant. Formulations were prepared containing Span 60 and cholesterol in 1:1 and 2:1 ratios, respectively, with essential oils added at increasing concentrations. The formulated niosomes had nano-vesicles with entrapment efficiency ranging from 75.81% to 91.25% and in-vitro drug release ranging from 80.61% to 89.81%. The optimal formulation was selected based on particle size, entrapment efficiency and in-vitro drug release. Optical microscopy and high-resolution transmission electron microscopy studies revealed a spherical shape of the niosomal vesicles. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction studies confirmed complete encapsulation of the drug in the niosomal vesicles. The optimized formulation was also incorporated into a gel base, which was then evaluated for appearance, pH, viscosity, spreadability, in vitro drug release and stability. Overall, the results indicated that the developed niosomal lacidipine vesicles may provide an alternative to existing delivery systems for this drug.

Despite numerous remarkable developments in clinical therapy, the world remains firmly in the grip of fungal infections. While conventional approaches to antifungal therapy are failing, dermatophytes continue to affect people’s daily lives, especially in humid and tropical areas, and pose a major medical problem. Cubosomes, the liquid crystalline nanostructures, are among the recently developed lipid nanoparticles that could potentially overcome the hurdles of conventional therapy. In the present study, cubosomes containing luliconazole, an antifungal drug, were formulated to overcome the limitation of poor water solubility and poor bioavailability of the drug for the main purpose of treating fungal infections. Various formulations of luliconazole loaded cubosomes were prepared with different ratios of lipid (glyceryl monooleate) and surfactant (poloxamer 407) using emulsification method. The prepared formulations were optimised and the optimised cubosomal dispersion was loaded into a carbomer-934 gel to form an emulsifying gel. All cubosomal dispersions had particle sizes ranging from 124 nm to 221.1 nm, optimal zeta potential and polydispersity index, and were found to be stable. The drug entrapment efficiency of the cubosomes was over 90%. The in vitro diffusion study showed that the developed formulation had a higher release rate than the marketed formulation. The in vitro antifungal activity study confirmed that the prepared emulsion formulation was also effective against Candida albicans. The novel drug delivery system developed in this study, the cubosomal emulgel, could thus be a favourable approach for the topical delivery of luliconazole for the treatment of fungal infections.

Ebastine, a histamine H1 antagonist, nonsedating, belonging to BCS class II is used in the treatment of allergic rhinitis and chronic idiopathic urticaria. The current study was intended in augmenting the aqueous solubility and dissolution rate of ebastine, by formulating a microemulsion system using oleic acid, Transcutol

Objective: The objective of the present work was to formulate and evaluate a fast-dissolving oral film of lurasidone hydrochlorideused as an atypical antipsychotic for the treatment of schizophrenia capable of providing faster onset of action. Methods: The fastdissolving films of lurasidone hydrochloride were prepared by the solvent casting technique using different compositions and combinations of hydroxypropyl methylcellulose E-3, E-5, E-15, and K4M as fast-dissolving polymer bases. A set of seven formulations were prepared and evaluated for parameters like physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance,tensile strength), surface pH, in vitro disintegration time, drug content, and an in vitro drug release. Results: The prepared films exhibited uniform and a smooth surface with uniform weight, thicknessand 89-90% mg drug content. The formulation F7 Showed excellent elasticity and disintegration within seconds. Lurasidone hydrochloride was rapidly released in vitro from all formulations. The release was found to be rapid and maximum of 41.5% in Phosphate buffer pH 6.8 and 58.6% in 0.1 N hydrochloric acid over a period of 30 min. The further optimized formulation F7Adepicted a faster and maximum release of 78% as compared to the marketed tablet 74%. Conclusion: The developed formulation is a better alternative to tablets by its ability to produce good drug release.

Objective: To overcome the limitations of fast dissolving tablets, a novel fast dissolving film of ebastine was formulated for attaining quick onset of action, aiding in the enhancement of bioavailability favorable in severe conditions of allergies. Methods: Films of ebastine were prepared by the solvent casting method using hydroxypropyl methylcellulose E-15, hydroxypropyl methylcellulose K-4 as a film base with different concentrations of crospovidone as superdisintegrant and polyethylene glycol-400 as a plasticizer. Further physical characteristics such as uniformity of weight, thickness, and drug content uniformity, tensile strength, folding endurance, percentage elongation, surface pH, disintegration and in vitro drug release were evaluated. Results: The optimized formulations with film base hydroxypropyl methylcellulose E-15 and hydroxypropyl methylcellulose K-4 containing 8% crospovidone showed 99.34 % and 97.42 % of maximum cumulative percentage release respectively exhibiting first order kinetics. However, no significant change was observed in stability studies. Conclusion: The concept of formulating fast dissolving films of ebastine offers a suitable approach in exhibiting rapid onset of action with improved delivery.

Background: The formulation of spanlastic vesicles of luliconazole can be used to overcome its poor skin permeation and improve its antifungal efficacy. Objective: In this study, we aimed to enhance the dermal delivery of luliconazole, an antifungal drug, through spanlastic vesicles. Methods: A 23 regular factorial design was employed, using the Design Expert® software for optimization. The independent variables chosen were Span: Edge activator ratio, type of edge activator, and sonication intensity and their effect on the dependent variables, i.e., entrapment efficiency, particle size, and percentage of drug release after 8h were determined. Spanlastics were formulated by ethanol injection method using Tween 80 as an edge activator. Results: Spanlastics were found to possess sizes in the nano range with entrapment efficiencies between 77 - 88% with optimum zeta potential and polydispersity index indicating a stable formulation. Differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared studies revealed complete encapsulation of the drug within the elastic carriers. The optimized spanlastic formulation was further incorporated into a gel base and was found to be sufficiently viscous, spreadable, homogenous, showed a prolonged release for up to 8h and was also found to be non-irritant. The in-vitro permeation study revealed that the flux value obtained for luliconazole entrapped in the vesicular spanlastics (0.2292 mg/cm2.h) was also found to be higher than that of the marketed (0.1302 mg/cm2.h) and conventional gel (0.1122 mg/cm2.h). The optimized gel formulation was also evaluated for its antimycotic activity. Moreover, the optimized gel formulation also possessed a greater antimycotic activity against Candida albicans. The spanlastics loaded hydrogel formulation was found to have a greater zone of inhibition in comparison to the marketed formulation, thus proving to have optimum antifungal activity against Candida albicans. Conclusion: Collectively, the results revealed that spanlastics could be a potential nanocarrier for wellcontrolled delivery and for targeting deeper skin layers, thus providing new opportunities for dermal treatment.

Ebastine (EBS) is a second-generation non-sedating antihistamine used for the prevention and treatment of allergic rhinitis and chronic idiopathic urticaria. It is BCS class II drug exhibiting low aqueous solubility and poor oral bioavailability. The present work was aimed at enhancing the dissolution rate of EBS by formulating it in the form of a liquisolid (LS) system using Tween 20 (non-volatile solvent), Avicel PH 102 (carrier material) and Aerosil 200 (coating material). Various batches of LS powder system were formulated by adopting a mathematical model for calculating required quantities of excipients. The absence of interaction between drug and excipients was checked by Fourier transform IR spectroscopy and differential scanning calorimetry studies. Formulated EBS tablets were evaluated for post compression parameters. X-ray powder diffraction studies and scanning electron microscopy showed the loss of EBS crystallinity in LS formulations. Formulation F9 was considered as optimum, showing a higher drug release of up to 99.06% in comparison to marketed tablet formulations. Stability of the optimized formulation was confirmed by results of the accelerated aging study. Thus, it is concluded that LS formulation is a favorable method of EBS solubility enhancement.

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.

Felodipine (FDP), a dihydropyridine calcium-channel antagonist is used for the treatment of hypertension and angina pectoris. FDP is poorly soluble drug and upon oral administration, it undergoes first pass metabolism, resulting in bioavailability of 15%. The present work was aimed to formulate rapidly dissolving strips containing FDP nanoparticles for transbuccal administration. Such formulations are absorbed through buccal mucosa resulting in increase in oral bioavailability by circumventing first pass metabolism. Nanosuspension was formulated using solvent-antisolvent sonoprecipitation technique. An ordinary 23 factorial design was applied using Design Expert® 12 software. Formulated nanosuspensions were characterized for particle size, polydispersity index, zeta potential and saturation solubility. Surface morphology was studied using high resolution transmission electron microscopy, atomic force microscopy and field emission scanning electron microscopy. The optimised nanosuspension D1 formulated with PVP-K30 as stabiliser was selected for further incorporation into the film. Central composite design was applied to select film composition with desirable properties. X-ray diffraction studies were performed to assess the solid-state characteristic of the drug in the formulation. Rapidly dissolving strips were evaluated for weight variation, folding endurance, disintegration time, thickness and surface pH. Scanning electron microscopy image of the optimised film revealed almost granular-shaped nanoparticles dispersed in the polymeric network. Drug release kinetics data of optimised film F5 showed 82 ± 0.47% release within 4 min and release pattern was non-fickian diffusion controlled. Stability studies were conducted at 25 ± 2 °C/60 ± 5% RH for 90 days. Collectively, the developed film demonstrated to possess optimum physical and mechanical properties along with rapid drug release and good stability.

Dermatophytes, a group of fungal species causing superficial fungal infections possess a major health problem in a wide group of people. Various approaches have been used in past for treatment of such infections but, owning to their low dermal permeability and less retention time, such formulations are proven to be less effective. Thus, to overcome such limitations, various novel drug delivery systems were developed. “Nanosponge” - a porous nano carrier system which can entrap drug of choice and improve its dermal availability, permeation rate and retention time is one such example. In the present study, a novel azole antifungal drug luliconazole, having wide spectrum of activity and potent against dermatophytes was used as model drug. It has low aqueous solubility and less dermal availability. A regular 2-level factorial design was applied using Design Expert® 11 software to formulate luliconazole loaded nanosponge drug delivery system using emulsion solvent diffusion method. Polyvinyl alcohol and ethyl cellulose were used as polymers. Formulated nanosponges were characterised for percentage entrapment efficiency, particle size, poly dispersibility index, zeta potential, surface morphology studies using scanning electron microscopy (SEM), transmission electron microscopy (TEM) and porosity. Fourier transform infrared spectroscopy, X-ray diffraction and differential scanning calorimetric analysis were also carried out to confirm the encapsulation of the drug within the carrier. In vitro release studies and other relevant parameters were also determined. Further, prepared nanosponges were incorporated into gel base using carbomer 934 and characterised for viscosity, swelling behaviour, spreadability, in vitro diffusion studies, skin irritancy test, in vitro permeation studies using rat skin membrane, antifungal activity and stability studies. From the results obtained it was evident that, formulated nano carriers were in desired nano size range having characteristic porous structure which was further confirmed by SEM and TEM studies. It was perceived that percentage drug entrapment efficiency was in the range of 70–80%. Drug release kinetics data revealed prolonged release up to 8 h. Release pattern was found to be diffusion controlled which was confirmed by Higuchi's plot. In vitro permeation studies revealed enhanced permeation rate and skin retention time. Collectively, the developed drug delivery system had greater permeation rate and increased retention time. Further, the formulation was found to be non-irritant and stable. Overall, the aim of enhancing dermal availability and sustaining the release of drug for effective fungal therapy was achieved by formulating as nanosponge gel.

Objective: The aim of the present investigation was to design and evaluate fast dissolving tablet (FDT) for the oral delivery containing solid dispersion of meclizine (MCZ) hydrochloride, an antiemetic drug. Methods: The solubility of meclizine was increased by preparing solid dispersions using mannitol as a carrier by fusion method. The prepared solid dispersion, was subjected for in vitro drug release, percent practical yield, drug content, infrared spectroscopy (IR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM). Optimized solid dispersion was incorporated to prepare fast dissolving tablets. Preformulation studies were carried out on tablet blends. The prepared solid dispersion, as well as pure drug fast dissolving tablets, was evaluated for drug content, weight variation, hardness, friability, in vitro drug release, wetting time, disintegration time, water absorption ratio, in vitro dispersion time. Results: Meclizine pure drug, solid dispersions formulations SD1, SD3 and SD5 showed 12.8, 31.68, 38.92 and 53.28% cumulative drug release in phosphate buffer pH 6.8 after 60 min, respectively. Thus faster dissolution rate was exhibited by the solid dispersion containing 1:5 (w/w) ratio of meclizine: mannitol. Percent cumulative drug release for control and solid dispersion tablets after 60 min in phosphate buffer pH 6.8 was 92.04 and 98.2% respectively. The release of drug meclizine from best formulation SD5 FDT was found to be faster than pure drug FDT. Conclusion: Fast dissolving tablet of optimized solid dispersion showed better in vitro dissolution result then FDT of pure drug at the end of one hour.