Proniosomal Gel Research Articles

Fabrication of Anti-HSV-1 Curcumin Stabilized Nanostructured Proniosomal Gel: Molecular Docking Studies on Thymidine Kinase Proteins

Curcumin is a dietary compound with accrued evidence of antiviral activity. Poor solubility and permeation renders curcumin a good applicant for incorporation into proniosomes. The intent of this study was to formulate curcumin proniosomal gel for topical application and the evaluation of its in-vitro, ex-vivo activities against Herpes Simplex virus type 1 (HSV-1), as well as molecular docking studies on HSV-1 thymidine kinase proteins. Coacervation phase separation tactic, using 23 full factorial design, was used in the preparation of different proniosomes. Cytotoxicity of the selected formulae (F4 and F8) was evaluated on the Vero cell line. Optimal formulae (F4 and F8) showed entrapment efficiency of 97.15 ± 2.47% and 95.85 ± 2.9%, vesicle size of 173.7 ± 2.26 nm and 206.15 ± 4.17 nm and percentages curcumin released after 3 h of 51.9 ± 1.4% and 50.5 ± 1.1%, respectively. Ex-vivo permeation studies demonstrated that the optimal formulae markedly improved the dermal curcumin delivery. Curcumin proniosomal gel formulae exhibited 85.4% reduction of HSV-1 replication. The ability of curcumin to interact with the key amino acids in the enzyme binding sites of 1KI7, 1KI4, and 1E2P, as indicated by its docking pattern, rationalized its observed activity. Therefore, curcumin proniosomes could be considered as a successful topical delivery system for the treatment of HSV-1.

Effect of Formulation Variables and Gamma Sterilization on Transcorneal Permeation and Stability of Proniosomal Gels as Ocular Platforms for Antiglaucomal Drug.

This study aims to evaluate the effect of different formulation variables (surfactant type and HLB value) adopting full factorial design (51. 21) using coacervation phase technique on in vitro characterization of dorzolamide hydrochloride (DZ)-loaded proniosomal gels, namely, entrapment efficiency percentage (EE%), vesicle size distribution, polydispersion index (PDI), and in vitro DZ release. The optimum formula F2 with a desirability value of 0.937 composed of 40mg DZ, 500mg span 60, 500mg of L-α-Lethicin, and 55.5mg cholesterol showing EE% of 84.5 ± 1.5%, PS of 189.5 ± 35.76nm with PDI 0.8 ± 0.28 and 58.51% ± 1.00 of DZ released after 8h was further evaluated using differential scanning calorimetry (DSC) and transmission electron microscopy (TEM). The effect of gamma sterilization on transcorneal permeation and stability of DZ from the selected formulation (F2) revealed that F2 was significantly tolerable, stable, and competent to corneal permeation confirmed by histological examination, confocal laser microscopy, and intraocular pressure (IOP) measurement. Significant corneal bioavailability was attained from formula F2 (370.6mg. h/m) compared to the market product Trusopt® eye drops (92.59mg. h/ml) following IOP measurement, thereby proniosomal gels could be considered as tolerable and competent ocular platforms for improving the transcorneal permeation of DZ.

Development and Evaluation of Optimized Thiolated Chitosan Proniosomal Gel Containing Duloxetine for Intranasal Delivery.

Proniosomes offer excellent potential for improved drug delivery, through versatile routes, by overcoming the permeation barriers faced by several drugs. The study was aimed to develop a thiomer gel containing duloxetine proniosomes for the intranasal delivery, improving its bioavailability and brain delivery through olfactory system. Duloxetine-loaded proniosomes were optimized through Design-Expert Software, prepared by coacervation phase separation method and then characterized in vitro for different vesicle features, and permeation enhancement potential using various techniques. The formulation F2, out of all the trials, fulfilled the maximum requisite of highest entrapment efficiency (76.21 ± 1.24%) and minimum vesicle size (223.91 ± 11.07nm). The F2 was embedded in thiolated chitosan gel rendering it mucoadhesive and further characterized. The in vitro release showed a sustained drug release from the mucoadhesive proniosomal gel with only 54% drug release as compared to that of 71% from proniosome over 8h, following Higuchi drug release model. Ex vivo permeation studies showed the enhancement ratio for the mucoadhesive proniosomal gel to be 1.86-fold greater than proniosomes, indicating a significant improvement in transmucosal permeation. The results suggest that incorporation of proniosomes into thiolated gel can significantly improve its mucoadhesion and retention time in the nasal cavity for providing a sustained drug release. Thus, gel formulation could be considered as a promising approach for efficient intranasal drug delivery of duloxetine. Graphical Abstract.

Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel

Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P < 0.001) from control and displayed steady and prolonged tramadol release by Fickian diffusion. Transdermal therapy of F4 showed prominent reduction of induced twitches (P < 0.005) in mice and edema (P < 0.05) in rats, as compared to oral tramadol. The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed. In conclusion, the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy.

FORMULATION AND EVALUATION OF PRONIOSOMAL GEL-BASED TRANSDERMAL DELIVERY OF ATORVASTATIN CALCIUM BY BOX–BEHNKEN DESIGN

Objective: The aim of this study was to investigate the combined influence of three independent variables in the preparation of atorvastatin proniosomes by coacervation-phase separation method.&#x0D; Methods: On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of cholesterol, soya lecithin, and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Transmission electron microscopy analysis of optimized formulation has demonstrated the presence of individual proniosomes in spherical shape.&#x0D; Results: Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency, and also, the drug release was 99.72% within 24 h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the drug release was followed by zero-order manner with Korsmeyer–Peppas model, which implies super case II release kinetics. The particle size and zeta potential of the optimized atorvastatin proniosomal gel were found to be 65.72 and −10.5, respectively. The optimized batch of proniosomes was used for the preparation of atorvastatin-based proniosomal hydrogel by incorporating hydrated proniosomes to carbopol matrix to enhance the stability and viscosity of the system.&#x0D; Conclusion: The enhanced skin permeation, for a prolonged period of time, may lead to improved efficacy and better patient compliance. This study suggests that proniosomal gel-containing atorvastatin could perform therapeutically better effects than the conventional formulations.

FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same.&#x0D; Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc.&#x0D; Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability.&#x0D; Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

FORMULATION DEVELOPMENT AND EVALUATION OF PRONIOSOMAL GEL OF ETHINYLESTRADIOL AND LEVONORGESTREL FOR ANTIFERTILITY TREATMENT

Objective: The purpose of this research was to develop and formulate proniosomal gel drug delivery system of ethinylestradiol and levonorgestrel for antifertility treatment that is capable of efficiently delivering entrapped drug over an extended period of time.Methods: Ethinylestradiol and levonorgestrel are encapsulated in various formulations of proniosomal gel composed of various ratios of span surfactant, cholesterol, soya lecithin, and alcohol as aqueous phase prepared by coacervation-phase separation method. The prepared formulations characterized for drug encapsulation efficiency, size distribution, in vitro release studies, and vesicular stability at different storage conditions were carried. Stability studies for proniosomal gel were carried out for a few weeks. Morphological size and shape of the vesicles are characterized using optical microscopy and scanning electron microscopy (SEM). Stability studies for proniosomal gel were carried out for 3 months.Results: Morphological size and shape of the vesicles are characterized using optical microscopy and SEM, particles are found to be spherical, size of the particles is in the range of 46.4–80.6 nm, and permeation studies showed good control release for prolonged period of time. The encapsulation efficiency of proniosomal gel formulations is in the range of 74–80% and in vitro permeation studies proved that good amount of drug is permeated and has reasonably good stability characteristics as well.Conclusions: The results suggest that proniosomal gel formulations of ethinylestradiol and levonorgestrel may be used for transdermal delivery for antifertility treatment. The dried proniosomal formulation could act as a promising alternative to niosomes.

FORMULATION DEVELOPMENT AND EVALUATION OF PRONIOSOMAL GEL OF ETHINYLESTRADIOL AND LEVONORGESTREL FOR ANTIFERTILITY TREATMENT

Objective: The purpose of this research was to develop and formulate proniosomal gel drug delivery system of ethinylestradiol and levonorgestrel for antifertility treatment that is capable of efficiently delivering entrapped drug over an extended period of time.Methods: Ethinylestradiol and levonorgestrel are encapsulated in various formulations of proniosomal gel composed of various ratios of span surfactant, cholesterol, soya lecithin, and alcohol as aqueous phase prepared by coacervation-phase separation method. The prepared formulations characterized for drug encapsulation efficiency, size distribution, in vitro release studies, and vesicular stability at different storage conditions were carried. Stability studies for proniosomal gel were carried out for a few weeks. Morphological size and shape of the vesicles are characterized using optical microscopy and scanning electron microscopy (SEM). Stability studies for proniosomal gel were carried out for 3 months.Results: Morphological size and shape of the vesicles are characterized using optical microscopy and SEM, particles are found to be spherical, size of the particles is in the range of 46.4–80.6 nm, and permeation studies showed good control release for prolonged period of time. The encapsulation efficiency of proniosomal gel formulations is in the range of 74–80% and in vitro permeation studies proved that good amount of drug is permeated and has reasonably good stability characteristics as well.Conclusions: The results suggest that proniosomal gel formulations of ethinylestradiol and levonorgestrel may be used for transdermal delivery for antifertility treatment. The dried proniosomal formulation could act as a promising alternative to niosomes.

RECENT UPDATE ON PRONIOSOMAL GEL AS TOPICAL DRUG DELIVERY SYSTEM

An existence of transdermal delivery tool, proniosomal gel, has established to showed remarkable development for lipophilic/hydrophilic drugs over additional formulations. Newer drugs of lipophilic nature emerge poor bioavailability, irregular absorption, and pharmacokinetic changes. Therefore, this novel drug delivery system has been proved advantageous over other oral and topical delivery of drug candidates to bypass such disruption. This proniosomal gel basically is a compact semi-solid liquid crystalline (gel) composed of non-ionic surfactants easily formed on dissolving the surfactant in a minimal amount of acceptable solvent and the least amount of aqueous phase and phosphate buffer. Topical application of gel under occlusive condition during which they are converted into nisomes due to hydration by water in the skin present itself. Proniosomal gels are typically present in transparent, translucent, or white semisolid gel texture, which makes them physically stable throughout storage and transport. This review provides an important overview of the preparation, formulation, evaluation, and application of proniosome gel as a drug delivery carrier.

RECENT UPDATE ON PRONIOSOMAL GEL AS TOPICAL DRUG DELIVERY SYSTEM

An existence of transdermal delivery tool, proniosomal gel, has established to showed remarkable development for lipophilic/hydrophilic drugs over additional formulations. Newer drugs of lipophilic nature emerge poor bioavailability, irregular absorption, and pharmacokinetic changes. Therefore, this novel drug delivery system has been proved advantageous over other oral and topical delivery of drug candidates to bypass such disruption. This proniosomal gel basically is a compact semi-solid liquid crystalline (gel) composed of non-ionic surfactants easily formed on dissolving the surfactant in a minimal amount of acceptable solvent and the least amount of aqueous phase and phosphate buffer. Topical application of gel under occlusive condition during which they are converted into nisomes due to hydration by water in the skin present itself. Proniosomal gels are typically present in transparent, translucent, or white semisolid gel texture, which makes them physically stable throughout storage and transport. This review provides an important overview of the preparation, formulation, evaluation, and application of proniosome gel as a drug delivery carrier.

Proniosomal gel-mediated topical delivery of fluconazole: Development, in vitro characterization, and microbiological evaluation.

The aim of this study was to explore the potential of proniosomal gel for topical delivery of fluconazole, an antifungal drug used in fungal infections caused by pathogenic fungi. Fluconazole-loaded proniosomal gels were prepared by the coacervation phase separation method using different nonionic surfactants (spans and tweens). The prepared fluconazole proniosomal gels were evaluated for various parameters such as particle size (PS), drug entrapment efficiency percentage (EE%), and in vitro drug release. The experimental results showed that the EE% for the prepared formulae are acceptable (85.14%–97.66%) and they are nanosized (19.8–50.1 nm) and the diffusion from the gels gave the desired sustaining effect. F4, which was prepared from span 60, tween 80 (1:1), and cholesterol showed highest EE% and gave slow release (40.50% ± 1.50% after 6 h), was subjected to zeta potential (ZP) test, transmission electron microscopy as well as microbiological study. The results showed a well-defined spherical vesicle with sharp boundaries with good physical stability of fluconazole within the prepared gel. Moreover, F4 showed an excellent microbiological activity represented by a greater zone of inhibition (5.3 cm) compared to control gel (fluconazole in 2% hydroxy propyl methyl cellulose (HPMC) gel formula) (4.2 cm) and plain gel with no drug (0 cm) against Candida albicans. This study showed the suitability of the proniosomal gel in attaining the desired sustainment effect for topical delivery of fluconazole for the management of fungal infection. The physical stability study showed that there was no significant change in EE%, PS, and ZP of fluconazole proniosomal gel after storage for 6 months.

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Brimonidine tartrate (BRT) is a hydrophilic α2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the entrapped drug. For this reason, BRT proniosomes were prepared to overcome niosomal instability issues. A D-optimal design was utilized to determine the optimum conditions for preparation of the proniosomal gels. Independent variables were amount of surfactant, surfactant:cholesterol ratio, and type of surfactant used. The dependent variables were entrapment efficiency (EE%), particle size, percentage of drug released after 2 h (Q2h), and percentage of drug released after 24 h (Q24h). The optimum formula was suggested with desirability 0.732 and the composition of 540 mg Span 60 and 10:1 surfactant:cholesterol ratio. The results obtained after reconstitution were; EE% of 79.23 ± 1.12% particle size of 810.95 ± 16.758 nm, polydispersity index (PDI) 0.6785 ± 0.213, zeta potential 59.1 ± 0.99 mV, Q2h40.98 ± 1.29%, Q8h 63.35 ± 6.07%, and Q24h = 91.11 ± 1.76%. Transmission electron microscope imaging of the formula showed the typical spherical shape of niosomes. In-vivo pharmacodynamic study assured the improved ocular bioavailability of BRT selected formula when compared with Alphagan®P with relative AUC0–24 of 5.024 and 7.90 folds increase in the mean residence time (MRT). Lack of ocular irritation of the formula was assured by Draize test.

FORMULATION AND EVALUATION OF ACECLOFENAC PRONIOSOME LOADED ORABASE FOR MANAGEMENT OF DENTAL PAIN

Objective: The main motive is to develop proniosomes loaded orabase for enhanced permeation and prolonged release of aceclofenac for oro dental conditions.Methods: Various aceclofenac (ACL) proniosomal gels were formulated employing various surfactants, span 60 was superior and significant for loading into orabase. The formulations were scrutinized for entrapment efficiency, optical microscopy, in vitro diffusion and release studies, mucoadhesive strength, ex-vivo permeation studies and drug-excipient interactions were determined by FTIR spectroscopy.Results: Considering best entrapment efficiency with span 60 (97.60±1.85) and optimum vesicle shape, along with prolonged drug permeation (45% for 24 h) the formulation F(ACL)1 was selected and optimized for loading into orabase. The F(ACL)1 loaded orabase exhibited significant prolonged release over 14 h, and permeation profiles exhibited nearly two-fold increased flux in comparison with control. Good mucoadhesive strength was observed for proniosomal orabase 6370 dynes/cm2. No evidence of incompatibility amongst formulation components from FTIR studies. SEM images revealed the particle size range from 136 µm to 236 µm for proniosomal orabase.Conclusion: Orabase can be an effective carrier for proniosomes with enhanced permeation and prolonged release for oro-dental conditions.

DESIGN OF PRONIOSOMAL GEL CONTAINING EUGENOL AS AN ANTIFUNGAL AGENT FOR THE TREATMENT OF ORAL CANDIDIASIS

The objective of this study was to design and investigate the antifungal activity of proniosomal gel of eugenol for the treatment of oral candidiasis. The proniosomal gel was prepared by coacervation phase separation method using different surfactants like spans 20, 60, 80, soya lecithin and cholesterol. The proniosomal gel formulations were evaluated for visual inspection, pH detection, viscosity, spreadability, in vitro drug release and kinetics study, and in vivo studies. The compatibility study indicated that the drug and the excipients were compatible with each other. The results showed that pH, viscosity and spreadability were all acceptable for topical preparation. In vitro drug release study and drug release kinetics were conducted to check the release study and drug release patterns of the formulation. Amongst the formulations, an optimized formulation was selected to conduct an in vivo study. Candida albicans was used to induce oral candidiasis for the evaluation of therapeutic efficacy of proniosomal gel in immunosuppressed rats. Activity was analysed by microbiological and histopathological techniques and was compared with the marketed product. It is evident from the study that the proniosomal gel shows sustained release trend with strong antifungal activity.

Formulation and In Vivo Evaluation of Proniosomal Gel Based Transdermal Delivery of Atorvastatin Calcium

Formulation and In Vivo Evaluation of Proniosomal Gel Based Transdermal Delivery of Atorvastatin Calcium

Development and Optimization of Lovastatin-loaded Trans-dermal Proniosomal Gel using Box-Behnken Design

In this study, a proniosome-based transdermal drug delivery system of lovastatin was developed by coacervation phase separation method. On the basis of the pilot trials, a 3-factor, 3-level Box–Behnken design was employed to characterize the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, entrapment efficiency, and drug release). TEM analysis of optimized formulation has demonstrated the presence of individual Proniosomes in spherical shape. Lovastatin optimized proniosomal formulation F1 shown better particle size and percentage entrapment efficiency and drug release of 99.49% within 24h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the systems predominantly released Lovastatin in a zero-order manner with a strong correlation coefficient (R2= 0.9990). The particle size and Zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged time may lead to improved efficacy and better patient compliance. &#x0D;

Development and in vivo Evaluation of Lovastatin Loaded Transdermal Proniosomal Gel by Design of Experiment

The objectives of the present study were to define effects on the hypercholesterolemia activity and pharmacokinetics of a novel transdermal proniosomal gel incorporating Lovastatin prepared by coacervation phase separation method. On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, % entrapment efficiency, and % of drug release). Lovastatin optimized proniosomal formulation F1 shown better particle size and % entrapment efficiency and drug release of 99.49% within 24 h in slow and controlled manner when compared with control. The particle size and zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin-based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. From in vivo studies the maximal concentrations (Cmax) of drug was significantly reduced while the areas under the plasma concentration–time curve (AUC) and t1/2 were evidently increased and extended. The results suggest that proniosomes can act as promising carrier which offers an alternative approach for transdermal delivery of Lovastatin. The study demonstrated the effectiveness of proniosomal preparation of Lovastatin for effective management of hypercholesterolemia to reduce risk of cardiovascular disease.

FORMULATION AND EVALUATION OF TOPICAL FORMULATION FOR CUTANEOUS TUBERCULOSIS

Cutaneous Tuberculosis is also known as dermal tuberculosis or tuberculosis cutis (extrapulmonary tuberculosis) which can occur in any age group and patients who may or may not be suffering from pulmonary tuberculosis. The current treatment given for the disease is oral therapy of anti-tubercular drugs which has many side effects such as hepatotoxicity, headache, anxiety, euphoria, insomnia, eosinophilia, hepatitis. Hence to avoid these side effects and to increase efficiency of current therapy a topical proniosomal gel of isoniazid was formulated. Coacervation phase separation method was used and proniosomal gel was formulated by using Span 20, soya lecithin, and cholesterol. Optimum concentration of 3 factors Span 20, soya lecithin, and cholesterol were determined using Box Behnken design with at 2 levels and vesicle size and entrapment efficiency as responses. The optimized proniosomal gel was characterized by vesicle size, entrapment efficiency, transmission electron microscopy (TEM), in vitro drug release, skin retention studies, skin irritation studies and stability studies. The optimised batch showed vesicle size of 2.27±1.82 µ, and entrapment efficiency of 98.15±0.25 %. The optimised formulation was stable under refrigeration condition (5°C) in amber coloured bottle, was non-irritating and showed 98.10±1.28 % release and 85±1.53 % permeation after 6 h and 436±12 µg drug was retained in the skin after 3 hrs. Keywords: Cutaneous tuberculosis, isoniazid, proniosomal gel, stabilityÂ

FORMULATION AND EVALUATION OF ANTIFUNGAL PRONIOSOMAL GEL FOR ORAL CANDIDIASIS

Fluconazole is a synthetic antifungal drug, belonging to triazole group and mostly used to treat oral candidiasis caused by the yeast Candida albicans. Fluconazole commercially available in tablets that offer poor bioavailability, due to hepatic first pass effect and gastric instability leads to frequent dosing. Buccal drug delivery can bypass such problems of tablet and leads to increase in bioavailability. Due to low molecular weight, fluconazole can suitably administered by buccal route, hence local and targeted action can achieve. The present study was conducted to develop proniosomal gel of fluconazole by coacervation phase separation method using Span 20, cholesterol, soya lecithin, ethanol and aqueous vehicle. Based on preliminary studies surfactant and aqueous vehicle was selected. The Box Behnken design was employed to optimized proniosomes by evaluating responses like entrapment efficiency, vesicle size and drug release. The optimized proniosomes were evaluated with entrapment efficiency (96.83%), vesicle size (2µm), in-vitro drug release 85.66 % (3 h) and ex vivo mucosal permeation (85.67 %) with flux (394.09 μg/cm2h). The optimized proniosomes were incorporated into 2% w/w Carbopol gel 934 (1:1) to obtain proniosomal gel. This optimized proniosomal gel was found with good viscosity, good spreadability and adhesiveness, also it shows maximum drug release and permeation as compared to plain gel of fluconazole. In microbiological studies, optimized formulation shows the maximum inhibitory effect as compared to plain gel of drug, which concluded that optimized proniosomal gel exerted local and targeted buccal delivery with good fungistatic effect than plain gel of fluconazole against Candida albicans. Keywords: proniosomal gel, oral candidiasis, fluconazole, mucoadhesion, Candida albicans.

BOX–BEHNKEN METHOD TO OPTIMIZE LORNOXICAM PRONIOSOMES: PREPARATION, IN VITRO CHARACTERIZATION AND ANALGESIC ACTIVITY

The objective of present investigation was to develop and evaluation of proniosomes as the carrier of lornoxicam for topical delivery. lornoxicam-loaded proniosomes were prepared by coacervation phase separation method. The Box–Behnken design used in this study helped in identifying the factors affecting drug entrapment efficiency and drug diffusion. Proniosomes were evaluated for appearance, pH, viscosity, entrapment efficiency and in vitro drug diffusion studies. The optimized formulations were further evaluated to vesicle size, shape, zeta potential, percutaneous permeation and analgesic effect. The vesicles were found to be unilamellar, spherical in shape. The analgesic effect of lornoxicam proniosomal gel showed better therapeutic activity.