Niosomal Gel Research Articles

Formulation and Evaluation of Niosomal Gel of Antifungal Luliconazole

Niosomes have potential applications in topical drug delivery system. Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and modify pharmacokinetic and bio-availability. Topically applied niosomes can increase the residence time of drugs in the stratum corneum and epidermis, while reducing the systemic absorption of the drug. It can act as drug containing reservoirs and the modification of the vesicular compositions or surface properties can adjust the drug release rate and the affinity for the target site. Luliconazole is a potential prescription candidate drug for the treatment of topical fungal infections. However, it has water solubility and skin permeability limitations. To overcome these limitations, a niosomal gel of luliconazole was formulated using Span 60, cholesterol and chloroform to improve its bioavailability and to reduce its toxicity. Niosomes were analyzed by transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FTIR) for morphological and spectral studies respectively. The formulations had ideal nanometric vesicle sizes, encapsulation efficiency (88.891% ± 0.0364%), Zeta potential (-40.1 mV), and storage instability was not observed. The sustained-release profile of niosomal gel was observed for up to 24 h. The highest R2 value was 0.913; the Higuchi model was considered the best fit model for the niosomal formulations. Based on the results, it can be concluded that niosomal luliconazole may enhance the activity of luliconazole against Candida albicans.
 Keywords: Luliconazole, Niosomes, Transdermal drug delivery, Antifungal drugs, Candida albicans

Ginger Extract-Loaded Sesame Oil-Based Niosomal Emulgel: Quality by Design to Ameliorate Anti-Inflammatory Activity.

Ginger, a natural plant belonging to the Zingeberaceae family, has been reported to have reasonable anti-inflammatory effects. The current study aimed to examine ginger extract transdermal delivery by generating niosomal vesicles as a promising nano-carrier incorporated into emulgel prepared with sesame oil. Particle size, viscosity, in vitro release, and ex vivo drug penetration experiments were performed on the produced formulations (ginger extract loaded gel, ginger extract loaded emulgel, ginger extract niosomal gel, and ginger extract niosomal emulgel). Carrageenan-induced edema in rat hind paw was employed to estimate the in vivo anti-inflammatory activity. The generated ginger extract formulations showed good viscosity and particle size. The in vitro release of ginger extract from niosomal formulation surpassed other formulations. In addition, the niosomal emulgel formulation showed improved transdermal flux and increased drug permeability through rabbit skin compared to other preparations. Most importantly, carrageenan-induced rat hind paw edema test confirmed the potential anti-inflammatory efficacy of ginger extract niosomal emulgel, compared to other formulations, as manifested by a significant decrease in paw edema with a superior edema inhibition potency. Overall, our findings suggest that incorporating a niosomal formulation within sesame oil-based emulgel might represent a plausible strategy for effective transdermal delivery of anti-inflammatory drugs like ginger extract.

Formulation and Evaluation of Azithromycin-Loaded Niosomal Gel: Optimization, In Vitro Studies, Rheological Characterization, and Cytotoxicity Study.

Several novel, innovative approaches for improving transdermal delivery of BCS class III drugs have been proposed. Despite their great aqueous solubility, BCS class III drugs have the drawback of limited permeability. The objective of the current work was to screen the suitability of niosomes as a nanocarrier in permeation enhancement of azithromycin (AZM) transdermal delivery. Niosomes were prepared by an ether injection method using a nonionic surfactant (Span 60) and cholesterol at different concentrations. The ζ potential (ZP), polydispersity index (PDI), and particle size (PS) of AZM-loaded niosomes were evaluated. The size of the niosomes was found to vary between 288 and 394 nm. The results revealed that the niosomes prepared in a ratio of 2:1 (Span 60: cholesterol) had larger vesicle sizes, but all of them were characterized by narrow size distributions (PDI <0.95). Niosomal gel was successfully prepared using different polymers. The appearance, pH, viscosity, and ex vivo drug release of niosomal gel formulations were all examined. The flow curves showed that the niosomal gel displayed lower viscosity values than its corresponding conventional gels. Niosomal and conventional gels exhibited a domination of the elastic modulus (G') over the viscous modulus (G″) (G'>G″) in the investigated frequency range (0.1-100 rad/s), indicating stable gels with more solid-like properties. Ex vivo skin permeation studies for the niosomal gel show 90.83 ± 3.19% of drug release in 24 h as compared with the conventional gel showing significantly lower (P < 0.001) drug release in the same duration (1.25 ± 0.12%). Overall, these results indicate that niosomal gel could be an effective transdermal nanocarrier for enhancing the permeability of AZM, a BCS class III drug. In conclusion, this study suggests that transdermal formulations of AZM in the niosomal gel were successfully developed and could be used as an alternative route of administration.

Thermoresponsive Azithromycin-Loaded Niosome Gel Based on Poloxamer 407 and Hyaluronic Interactions for Periodontitis Treatment

Azithromycin (AZM) is a potential antimicrobial drug for periodontitis treatment. However, a potential sustained-release system is needed for intra-periodontal pocket delivery. This study focused on the development and evaluation of a thermoresponsive azithromycin-loaded niosome gel (AZG) to search for a desirable formulation for periodontitis treatment. AZG was further developed from an AZM-loaded niosomal formulation by exploiting the advantages of poloxamer 407 (P407) and hyaluronic acid (HA) interactions. The results showed that the addition of HA decreased the gelation temperature and gelation time of AZG. HA was found to increase the viscosity as well as mucoadhesive and tooth-root surface adhesive properties. The AZG solution state was injectable and exhibited pseudoplastic shear-thinning behavior. P407–HA interactions in AZG could contribute to gel strength. AZG showed 72 h of continuous drug release following the Korsmeyer–Peppas model and potentially enhanced drug permeation. The formulations apparently presented more efficient antibacterial activity against major periodontal pathogens than the standard AZM solution. AZM intra-periodontal pocket formulation and the remarkable properties of niosomes exhibited potential characteristics, including ease of administration, bioadhesion to the anatomical structure of the periodontal pocket, and sustained drug release with competent antimicrobial activity, which could be beneficial for periodontitis treatment.

Optimization of clobetasol propionate loaded niosomal gel for the treatment of psoriasis: Ex vivo and efficacy study

Psoriasis is a chronic autoimmune inflammatory skin disease treated using corticosteroids. The current topical therapy is very challenging owing to the physicochemical nature of corticosteroids and thick psoriatic stratum corneum. In this paper, clobetasol propionate-loaded niosomal gel was tailored to increase drug permeation and deposition (high local drug concentration) in the psoriatic area for effective management of psoriasis. Thin film hydration technique and sonication was used to formulate niosomal gel using Span 60, cholesterol 934 (as gelling agent). Size (188 nm) and entrapment efficacy (78%) of the niosomes were optimized using Box Behnken design (BBD) approach by selecting cholesterol = 261.6 mg, Span 60 = 1.49% and sonication time = 8.6 min. The optimized niosomal gel showed acceptable size (188 ± 6 nm), zeta potential (−38 ± 6 mV), and viscosity (8521 ± 121 cp) for topical application. The ex vivo permeation profile showed high permeability of niosomes (61.12 ± 1.89% in 24 h) compared to marketed clobetasol propionate cream USP (8.56 ± 2.5% in 24 h). Niosomal gel showed 5.1-fold improvement in drug deposition in stratum corneum and viable layers compared to marketed cream. Fluorescence study indicates high localization of vesicular system in the skin layers. Further, in imiquimod-induced psoriatic model, the PASI (psoriasis area severity index) was significantly decline (better efficacy) with gel compared to marketed cream. Thus, the data demonstrated the potential of niosomal gel to improve drug permeation and deposition in the affected skin for effective management of psoriasis.

Formulation, evaluation, and in vitro drug diffusion of niosomal gel of selected drug

Aim: To minimise toxicity and alter pharmacokinetic and bioavailability, niosomes are becoming more significant in medication delivery. Rheumatoid arthritis, juvenile rheumatoid arthritis, and degenerative joint disease may benefit from this new non-steroidal anti-inflammatory, antipyretic, and analgesic drug. Materials and Methods: Non-ionic surfactants (Span 40, 60, and Tween 60) and cholesterol were used in various ratios to create tolmetin sodium niosomes in a thin film hydration process (CHO). Evaluations of the formulations were conducted in terms of size, shape, encapsulation efficiency, and in vitro drug release. Results: In vitro drug release ranged from 94.87±0.45 to 93.19±0.45 percent in 24 hours for niosomes that looked spherical in entrapment efficiency. Incorporating Tolmetin sodium niosomes with Span 60 and CHO in the ratio of 1:2.1 into Carbopol gel was shown to be promising. Tolmetin drug noisome has a drug content and pH of 99.19±1.20 and 7.0±0.06, respectively. Conclusion: An improved bioavailability gel formulation with Tolmetin sodium in niosomal form demonstrated longer effect than gel formulations containing Tolmetin in non-niosomal form.

Formulation and evaluation of niosomes-based chlorpheniramine gel for the treatment of mild to moderate skin allergy

Purpose of present study was to develop eight formulations of chlorpheniramine (CPM) niosomes according to 23 factorial design, characterise on the basis of various evaluation tests, i.e. in vitro drug release, SEM, FTIR, TGA and release kinetics, optimise the eight formulation on the basis in vitro drug release data, formulate gel of optimised dispersion, and to perform in vivo and histopathological study using gel of optimised dispersion on rabbits. Here, N3 having low level of cholesterol and span-80 but high level of span-60(0.1:0.2:0.05) was selected as optimised dispersion of niosomes that showed highest drug release i.e. 88.25% at pH 6 over 24 h of study and followed Korsmeyers-Peppas release kinetics with Fickian diffusion mechanism. After application of statistic by Analysis of variance (ANOVA) with 3D surface plots construction, gel of optimised dispersion of CPM niosomes was formulated, and evaluated by tests for i.e. viscosity, Spreadability, Extrudibility, drug content, drug entrapment, stability, SEM, FTIR, TGA, in vitro drug release, in vivo drug release following first order kinetics and histopathological study. Niosomal gel of CPM ensured successful development using suitable combination of non-ionic surfactants, and effective loading of drug for targeted delivery of drug.

Green formulation, characterization, antifungal and biological safety evaluation of terbinafine HCl niosomes and niosomal gels manufactured by eco-friendly green method

Terbinafine (TER) is a promising candidate medication for the topical treatment of fungal infections. However, its solubility in water and skin permeability are limited. To overcome these limitations, a Terbinafine niosome and niosomal gel was developed. The impact of cholesterol:surfactants on terbinafine incorporated niosome (terbinasome) preparations was examined. Differential scanning calorimetry (DSC), photon correlation spectroscopy (PCS), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy were used to assess the morphological features of terbinasome and the physicochemical characteristics of TER in terbinasome. The obtained results has shown that Chol enhanced the diameter of the terbinasome from 123.20 ± 2.86 to 701.93 ± 17.72 nm. The highest encapsulation of terbinafine was estimated to be around 66% due to the cholesterol:surfactants ratio in the terbinasome was 1:3 and 1:6. Additional examination has revealed that changes in the cholesterol:surfactants ratio can result in a change in the PDI value of between 0.421 ± 0.004 and 0.712 ± 0.011. The terbinasome gel was prepared and tested for pharmaceutical testing, including pH, viscosity, spreadability, and stability. The percentage of TER dissolution from terbinasome were determined more than 80% and showed quickest drug release. In a cutaneous permeability examination, the quantity of TER in the cutaneous layers and the receiver compartment were higher for the terbinasome gel than for the TER simple gel. The terbinasome's cell viability was around 90% (HFF cell line) and MTT experiment demonstrated that the terbinasome was not cytotoxic. The MIC of the terbinasome was lower than pure drug against Aspergillus, Fusarium, and Trichophyton. The terbinasomal gels were non-irritant (score < 2) in the cutaneous irritation examination performed on Wistar rats. The research suggests that the optimized terbinasome may be used as a nano-vesicle for TER drug administration, hence opening up new possibilities for the treatment of cutaneous infections.

Niosomal and ethosomal gels: A comparative in vitro and ex vivo evaluation for repurposing of spironolactone

The reported antiandrogenic effects of Spironolactone (Spn) provide a useful approach to be used off-label for treatment of androgenic alopecia (Aga). The aim of this study was to compare the efficiency of niosomes and ethosomes as carriers for the improved skin permeation of Spn. Spn-loaded niosomes and ethosomes were prepared and characterized by transmission electron microscopy, dynamic light scattering, Fourier-transform infrared spectroscopy and differential scanning calorimetry. Additionally, entrapment efficiency and in vitro release % were determined. The selected formulations (N1 and E14) were then incorporated into a hydroxypropyl methylcellulose -K4M (HPMC-K4M) gel base (2% w/w) and evaluated for drug permeation and skin deposition using abdominal rabbit skin. Spn-loaded niosomes and ethosomes displayed nanosized spherical morphologies with higher entrapment efficiency for niosomes (95–97.3%) than that for ethosomes (61.5–96.9%). Ex-vivo permeation studies for 24 h demonstrated superior Spn permeation from the ethosomal (Etho) gel (2.17-folds increase) when compared with the niosomal (Nio) gel. In conclusion, Spn can be successfully prepared as ethosomal gel with acceptable skin permeation and deposition properties which could be a promising new dosage form for off-label use of Spn for further clinical studies on management of Aga.

Preparation and Evaluation of Niosomes for the Delivery of Antioxidant to the Skin for Antiaging Purpose

Niosomes are unilamellar or multilamellar vesicles capable of entrapping hydrophilic and hydrophobic solutes. Niosomes are promising drug carriers as they possess greater stability. Niosomes is currently reported to increase drug stability, and increase the penetration of the adsorbed compound across the skin. Thus noisome could be incorporated in semisolid formulation. Quercetin niosomes were prepared by using Cholesterol, Span 80/ Span 85 as surfactants, chloroform, and diethyl ether using ether injection method. Formulation was then evaluated for particle size, drug content, entrapment efficiency, and in-vitro drug release studies. Niosomal Gel Prepared by Carbopol 934P and characterized as Drug Content, in-vitro Cumulative Drug Release and viscocity. Quercetin released from the Plain Gel to 68.64 in 8 hrs. The skin permeation increase of quercetin drug was recorded from vesicle Gel in comparison to plain gel and antioxidant activity performed by DPPH Method. The results showed that quercetin has considerable whitening and antioxidant capacities and Span80+85(1:2) Niosomes remarkably improved the solubility and photostability of quercetin. Furthermore, compared to quercetin solution, quercetin-niosomes had the advantages of sustained release and improved transdermal penetration. Niosomal Gel storage under refrigeration showed greater stability. The results suggested that Niosomes could better promote the transdermal delivery of quercetin, by their ability to control drug release.&#x0D;

Development and characterization of niosomal gel of fusidic acid: in-vitro and ex-vivo approaches

ABSTRACT Niosomes are multilamellar vesicles that efficiently deliver active substance into skin systemic circulation or skin layers. They are used in topical drug delivery system to enhance the skin permeation of active substance. So, the prime objective of this study was to develop a niosomal gel of fusidic acid to increase its skin permeation. Different formulations of niosomes of fusidic acid were designed by varying the cholesterol to surfactant ratio. Formulations containing fusidic acid, cholesterol, dihexadecyl pyridinium chloride, Span 60, or Tween 60 were prepared by thin film hydration method in rotary evaporator. The thin film formed in rotary flask was hydrated by phosphate buffer saline of pH 7.2. The niosomes formed were characterized through entrapment efficiency, size, polydispersity index (PDI), and zeta potential. The S3 formulation containing span 60 showed the highest entrapment efficiency (EE) of niosomes, so it was incorporated into Carbopol gel. Determination of pH, spreadability, rheological, and ex vivo permeation studies was conducted of niosomal gel. The results of ex vivo permeation studies showed high permeation of fusidic acid when gel was applied to an albino rat skin. According to the results and previous studies of niosomes, it can be concluded that niosomes enhanced the permeation of fusidic acid through the skin.

A comparative study of niosomal and elastic niosomal carbomer hydrogel for transcutaneous vaccine delivery

Transcutaneous immunization is becoming an attractive non-invasive vaccination strategy, though it is still challenging. This study evaluates the potential of transcutaneous delivery of antigens in mice through niosomal and elastic niosomal carbomer hydrogels. Ovalbumin was encapsulated into niosomes prepared by Span 80/cholesterol/stearylamine through reverse-phase evaporation. Ethanol was added into niosomal mixtures for elastic niosomes formation, then embedded in carbopol 934 hydrogel. Encapsulation efficiency and other physiochemical properties of the prepared niosomal vesicles such as particle size, stability, in vitro release and cytotoxicity were determined. In vivo immunizations of niosomal and elastic niosomal gel were carried out in mice. The optimal niosomal formulation loads 48.6 ± 5.2% ovalbumin with a vesicle size below 300 nm. A simple BCA method was used to determine the encapsulation efficiency of niosome. The cumulative permeation of proteins of niosomal gel was 15~20%. Both gels were stable at room temperature; however, elastic niosomal gel deteriorated at 60 ℃. Compared to free antigen, the topical administration of niosomal or elastic niosomal gel to mice displayed significant IgG titers. From the findings, compared to elastic niosomal gel, the niosomal hydrogel platform exhibited enhanced antigen delivery. Therefore, niosomal hydrogel may be considered a promising transcutaneous antigen delivery carrier.

Physicochemical Evaluation and Formulation of Propranolol Niosomal Gel with a Potential Effect on Infantile Hemangioma

Introduction: Propranolol is a non-specific beta-blocker that is used to treat hypertension, angina, arrhythmia, tremor, and manage thyrotoxicosis. Based on the results of various studies, propranolol can control infantile hemangioma by vasoconstriction, apoptosis induction, and inhibition of cell proliferation signals. Methods: The conventional film hydration method was used to prepare medium size (2-6 m) multilamellar vesicles (MLVs) containing propranolol. At the lipid phase, sorbitan esters (Spans) and their polyethoxylated derivatives (Tweens) were combined with cholesterol, and deionized water was utilized as a hydration medium. Laser light scattering was used to perform the size analysis, and the Franz diffusion cells were utilized to investigate the release of propranolol from niosomal suspensions and carbomer-based niosomal gels. The vesicles were assessed for their stability within six-month storage at 4°C, and ultraviolet spectrophotometer and centrifuge technique were employed to measure the efficiencies of encapsulation. Results: Based on the findings, the best niosomes were obtained at 40 and 60 spans in the presence of Tween 40 and 60; however, Span/Tween 20 and 80 were not able to form propranolol niosomes. The selected formulations had an MLV appearance and size distribution of 5 μm. Encapsulation efficiency and release rate of selected niosomes were optimal. Niosomes had good stability during six months of storage at refrigerator temperature. Conclusions: Based on the obtained results in this study, the application of a new topical dosage form of propranolol showed promising results for the treatment of infantile hemangioma

Sustained transdermal delivery of human growth hormone from niosomal gel: in vitro and in vivo studies

Human growth hormone (hGH) is widely used to treat several diseases for decades. However, the current treatment regime requires frequent injections via subcutaneous route due to short in vivo half-life, which leads to pain and poor patient compliance. In this study, a novel transdermal (non-invasive) hGH loaded niosomes gel was prepared to reduce the frequency of subcutaneous injections and to improve the patient compliance. Niosomes were prepared by film hydration technique at three levels of cholesterol. The particle size and entrapment efficiency increases with an increase in the level of cholesterol. Transmission electron microscopy images confirmed the spherical shape of niosomes without aggregation. Texture profiles analysis indicates that the niosomal gel has the required mechanical properties for transdermal application. The ex vivo permeation profile showed sustain hGH release for 4 days from the niosomal gel compared to 24 h from the control gel without niosomes. A rabbit skin irritation study showed no sign of irritation after application of niosomal gel. The pharmacokinetic parameters in the rat model showed 7.22-fold higher bioavailability with niosomal gel compared to control gel. In conclusion, the study demonstrated the potential of niosomal gel as an effective long-term sustained release strategy for hGH delivery to replace traditional subcutaneous injections.

Magnesium ascorbyl phosphate vesicular carriers for topical delivery; preparation, in-vitro and ex-vivo evaluation, factorial optimization and clinical assessment in melasma patients

Ascorbic acid (vitamin C) is an antioxidant that is widely used in cosmetics in skincare products. Due to the excessive low stability of ascorbic acid in cosmetic formulations, the stabilized ascorbic acid derivative, magnesium ascorbyl phosphate (MAP) was formulated as vesicular carriers; ethosomes and niosomes. The aim was to deliver MAP at the intended site of action, the skin, for sufficient time with enhanced permeation to get an effective response. Ethosomes were formulated using a full 32 factorial design to study ethanol and phospholipid concentration effect on ethosomes properties. Niosomes were formulated using 23 factorial designs to study the effect of surfactant type, surfactant concentration and cholesterol concentration on niosomes properties. The prepared formulations were evaluated for their Entrapment efficiency, particle size, polydispersity index, zeta potential and % drug permeated. The optimized ethosomal and niosomal formulations were incorporated into carbopol gel and evaluated for their permeation, skin retention and stability. A comparative split-face clinical study was done between the ethosomal and niosomal formulations for melasma treatment using Antera 3 D® camera. The optimized ethosomal and niosomal gels showed comparable controlled permeation and higher skin retention over their ethosomes and niosomes formulations respectively. Magnesium ascorbyl phosphate ethosomal gel showed clinically and statistically significant melanin level decrease after one month while MAP niosomal gel showed clinically and statistically significant melanin level decrease after six months. A combination of MAP ethosomes and niosomes could be promising skincare formulations for melasma and hyperpigmentation short and long-term treatment.

Formulation and Characterization of Nigella Sativa Niosomal Gel for Topical Application

Formulation and Characterization of Nigella Sativa Niosomal Gel for Topical Application

Niosomal formulation of hydroxytyrosol, a polyphenolic antioxidant, for enhancing transdermal delivery across human cadaver skin

Hydroxytyrosol (HT), a naturally occurring polyphenol from the olive plant, is a potent antioxidant, cardioprotective, neuroprotective, and anti-inflammatory agent. Upon oral administration, HT undergoes rapid elimination within minutes and thus limiting its therapeutic utility. Due to its hydrophilic nature, percutaneous absorption and transdermal delivery of HT are very low. The aim of this research was to enhance the skin permeation of hydroxytyrosol using a niosome gel formulation. The formulations prepared with Span 60 as surfactant showed uniform particle size and high encapsulation efficiency (>90%). The niosome formulations showed a pseudoplastic behavior for topical application within the lipid/surfactant composition of 45–50%. The formulations showed a controlled release of HT compared to the HT solution. The flux of HT across human skin was increased by 28 and 4.4 fold compared to aqueous and ethanolic HT solutions, respectively (p < 0.001). The presence of lecithin lowered the flux and increased the retention of the formulations compared to HT solutions (p < 0.001). The formulations containing lecithin showed two-fold higher skin retention of hydroxytyrosol (p < 0.05). In conclusion, this study demonstrates niosome gel as a promising alternative to oral delivery of HT, providing sustained delivery and greater efficacy.

Pharmacokinetic investigation of nitrendipine encapsulated niosomal gel in rat plasma by RP-HPLC method

The investigation was intended to develop niosomal gel and determination of bioavailability of nitrendipine by pharmacokinetic method via using Albino Wistar rats. The drug nitrendipine carries the least bioavailability after oral administration of about 10–20% due to the first pass effect thus niosomes encapsulated with nitrendipine drug were prepared for transdermal application to avoid the problem associated with oral administration. Niosomes were prepared by method of film hydration using cholesterol and span 60 and further incorporated into gel base to prepare niosomal gel. A sensitive and suitable method for the investigation of nitrendipine in the plasma of rat was developed using RP-HPLC. The process involves nitrendipine extarction in dichloromethane/sodium hydroxide, using reversed phase HPLC using a Shimadzu, Japan (SPD-M20A), (C18, 250 × 4.6 mm, 5 µm particle size, Phenomenex) column and at 238 nm UV detection. The niosomes were found with 226 nm size and found homogenous after incorporating into the matrix of gel with optimum pH of 6.2. The various pharmacokinetic parameters Cmax (0.716 ± 0.058 µg/ml), Tmax (12 hrs), t1/2 (21.23 ± 0.65 hrs), AUC o-infinity (26.15 ± 3.76 µg/ml. hr), AUC o-t (19.593 ± 2.22 µg/ml. hr), mean residence time (MRT: 34.81 ± 1.58 hrs) confirmed improved bioavailability of nitrendipine drug after transdermal application compares to oral administration.

Development and Characterization of Niosomal Gel for Topical Delivery of Luliconazole

Development and Characterization of Niosomal Gel for Topical Delivery of Luliconazole

Formulation and In Vitro Evaluation of Niosomal Gel of Loratadine: A Novel Topical Agent for Allergic Skin

Loratadine is an efficacious, non-drowsy antihistaminic molecule prescribed for allergic skin. The conventional oral dosage form is associated with various side effects, limited and variable absorption. The present study attempts to improve the effectiveness of the drug by formulating a niosome loaded hydrogel of loratadine for treating allergic skin. Ether injection method was used to prepare the niosomes of loratadine using Box Behnken design. Particle size analysis, surface charge, surface morphology (atomic force microscopy), compatibility (Fourier transform infrared spectroscopy), thermal (differential scanning calorimetry), and surface characteristics (powder X-ray diffraction) study were done to evaluate the drug-loaded niosomes. The optimized formulation was incorporated into two types of gelling systems. The nanogels were evaluated for rheological and mechanical properties, in vitro, ex vivo permeation and skin irritation studies. The Box Behnken design was found to be productive for the formulation of nano-sized (109.99 nm) and stable -37.5 mV niosomes of loratadine. The atomic force microscopy study revealed the formation of unilamellar niosomes, no incompatibility was detected between drug and excipients through Fourier transform infrared spectroscopy study. The differential scanning calorimetry and powder X-ray diffraction study reported the confinement of drugs in the niosomal core. The nanogels had good rheological and mechanical properties. The ex vivo study revealed the maximum penetration of the drug from the gel base of Xanthan gum, and no skin irritation was reported from the nanogel. The formulation and evaluation of niosomal gel of loratadine were found to have satisfactory permeation and can be a promising alternative approach for the administration of loratadine in the treatment of skin allergy.