Carbopol 934P Research Articles

DESIGN AND DEVELOPMENT OF LULICONAZOLE LOADED MESOPOROUS SILICA NANOPARTICLES AS HYDROGEL FOR MYCOTIC DISEASES

The aim of the present work was to design and synthesize of mesoporous silica nanoparticles as topical hydrogel formulation for inclusion of poorly water soluble antifungal drug like Luliconazole as a drug delivery platform. The SBA-15 was prepared to evaluate its application as a carrier for Luliconazole drug delivery. Its molecular size was suitable for incorporation in to the mesoporous of the SBA-15 materials. The SBA-15 was characterized by FTIR, UV analysis, Particle size, Transmission electron microscopy. The Synthesized Mesoporous silica i.e. SBA-15 was of mean particle size of 15 nm and specific area 283.763m2/g respectively. The results revealed that prepared mesoporous silica have small particle size, high surface area, and enhanced drug dissolution rate. The results obtained showed that Luliconazole was loaded with great efficiency into the SBA-15 which leads to enhanced diffusion of drug. Luliconazole hydrogel formulations improved medication permeation across the skin appropriate polymer was used to produce the formulation (Carbopol 934p and HPMC). The physiochemical parameters of all the established luliconazole formulations were assessed, including gel appearance, pH, viscosity, spreadability, globule size, Zeta potential, and drug content. Many of the above parameters yielded positive outcomes but F1 and F3 batch results was were unacceptable ranges. It can be assumed that the formulation F1 and F3 resulted in improved spreadability, stability, and homogeneity, as well as a stronger drug release analysis.

Clotrimazole Loaded Topical Gels: Formulation, Development and In-vitro Evaluation

The present study aimed to formulate and evaluate clotrimazole topical gel. Clotrimazole topical gel was prepared by dispersion method by utilizing various gelling agents like Carbopol 934p, HPMC K100, and Sodium alginate in three different ratios to achieve desired drug release. Prepared six gel formulations of clotrimazole were evaluated for pH, Viscosity, Drug content, Drug diffusion studies, and Drug release kinetic studies. The Drug-polymer compatibility reports have been done by FTIR absences of extraneous interactions among excipients. CTZGF4 releases 99.53% of the drug at the end of 8 hours and was considered as the best formulation. Therefore, formulations containing Carbopol produced better results than other formulations.

Implementation of Quality by Design Principles for the Evolution of Optimized Sustained Release Drug Delivery System

Aim: The aim of the present work is the implementation of Quality by Design principles for the evolution of optimized sustained release drug delivery system. Background: Quality by Design (QbD) approach refers to an advance approach to develop an optimized dosage form. QbD has become a vital modern scientific approach to develop a quality dosage form. In the modern era of science, researchers can develop an optimized dosage form with least effort, money and manpower. Objectives: Objective of the research work was the successful development of optimized floating bioadhesive tablets of glipizide using floating-bioadhesive potential of cellulosic polymer and carbomersusing quality by design (QbD) approach. Methods: Quality Target Product Profile (QTPP) of drug delivery system was defined as well as critical quality attributes (CQAs) were identified. A face centered central composite design (CCD) was utilized in assessing the impact of the individual critical material attribute (CMA) like Hydro Propyl Methyl Cellulose K4M(HPMC K4M)and Carbopol 934P (CP 934P) and their interactions, using least experimentation. Formulations were developed and quantitative impact on CQAs was determined using mathematical model. The optimized formulation was obtained and characterized for in-vitro as well as in-vivo parameters. Results: A Fishikawa diagram and Failure Mode and Effect Analysis (FMEA) was performed to identify potential failure modes associated with the dosage form. The optimum formulation was embarked upon using mathematical model developed yielding desired CQAs followed for confirmation of data. Sustained release drug delivery system was successfully developed by using QbD approach. In-vivo X-ray imaging in rabbit and γ-scintigraphic study in manconfirmed the buoyant nature of the mucoadhesive floating tablet for 8 h in the upper gastrointestinal tract. Conclusion: Optimized formulation shows phenomenal floating, bioadhesive properties and drug release retardation characteristics, utilizing a mixture of cost-effective polymers Hence, QbD approach may be regarded as an important tool in development of floating bioadhesive CR dosage forms.

Emulgels Containing Propolis and Curcumin: The Effect of Type of Vegetable Oil, Poly(Acrylic Acid) and Bioactive Agent on Physicochemical Stability, Mechanical and Rheological Properties.

Emulgels are obtained by the entrapment of an organic phase within a three-dimensional network built by hydrophilic molecules. Polymers based on cross-linked poly(acrylic acid) have been utilized as gel matrices, improving adhesiveness, rheological and mechanical performance. Propolis (PRP) produced by Apis mellifera L. bees displays a wide range of biological activities. Together with curcumin (CUR), they may show synergic anti-inflammatory, antioxidant and antimicrobial action on skin disorders. This work investigated the effect of vegetable oils (sweet almond, andiroba, and passion fruit) with regard to the physicochemical properties of emulgels composed of Carbopol 934P®, Carbopol 974P®, or polycarbophil aiming the CUR and PRP delivery. Physicochemical stability enabled the selection of systems containing passion fruit or andiroba oil. Mechanical and rheological characteristics provided rational comprehension of how vegetable oils and bioactive agents affect the structure of emulsion gels. All formulations exhibited high physiochemical stability and properties dependent on the polymer type, oil, and bioactive agent. Formulations displayed pseudoplastic, thixotropic and viscoelastic properties. Emulgels containing andiroba oil were the most stable systems. Carbopol 934P® or polycarbophil presence resulted in formulations with improved smoothness and mechanical properties. Systems containing andiroba oil and one of these two polymers are promising for further investigations as topical delivery systems of CUR and/or PRP on the skin and mucous membranes.

TOPICAL GEL OF EXTRACT OF MANGIFERA INDICA L. SEED KERNELS; AN INDIGENOUS PLANT WASTE FOR POTENTIAL ANTI-ACNE ACTIVITY

The present study was aimed at the development of topical gel of extract of Mangifera indica L. seed kernel and evaluation of its in vitro antibacterial activity. Various extracts using different solvents were prepared and evaluated for in vitro activity against Propionibacterium acnes. Ethanolic extract of M. indica L. seed kernel exhibited the highest in vitro antimicrobial activity and was considered further. Topical gels of this ethanolic extract were prepared using different polymers such as Carbopol 974P, Xanatural 180 and Methocel K15M in varying concentrations. The topical gel of 10 % w/w ethanolic extract of M. indica L. seed kernel with 2% w/w Carbopol 974P was uniform and yellowish transparent with satisfactory spreadability. The developed gel showed greater in vitro antimicrobial activity as compared to marketed herbal cream. These results indicate the potential of topical gel of ethanolic extract M. indica L. seed kernel as anti-acne formulation developed from plant waste product.

Acitretin Loaded Nanocarrier Gel: Formulation and Exploration of In-vitro Release Kinetics

Background: The present study intended to design and evaluate Acitretin (ACT) loaded Nanostructured Lipid Carriers (NLCs) for the management of psoriasis through topical application. Psoriasis is an autoimmune disorder that affects the skin and is characterized by irritation, red flaky patches over different parts of the body. ACT is an analog of vitamin A that is used for the management of psoriasis via the oral route. The prime demerit associated with oral route delivery of a drug is the teratogenic effect associated with the active molecule and side effects like dry mouth, runny nose, hair loss, taste changes, chapped lips, etc. that are the major contributing factors of reduced patient compliance. Objective: The objective of the present research work was to develop a topical formulation of ACT. Developing topical formulation for the same can result in enhanced patient compliance and can be worth compared to the marketed oral formulation of the drug. Methods: ACT loaded NLCs were prepared by hot homogenization method using oleic acid as a liquid lipid and stearic acid as a solid lipid in a 7:3 ratio along with the combination of a non-ionic surfactant (Tween 80) and an anionic surfactant (sodium lauryl sulphate). Results: In several optimization experiments, formulation F3 was found to be most appropriate for formulating gel. Morphological information obtained from SEM reinforced the formation of particles with nearly spherical morphology. The optimized formulation had a mean diameter of 363 nm, as founded by Zetasizer. XRD studies affirmed that the formulation exhibits amorphous nature, which is an essential character of NLC. An optimized formulation was further incorporated in the gel by using Carbopol 940P as a gelling agent. In vitro release studies indicated 96.85 ± 2% release in 8 hours with Korsmeyer- Peppas model release kinetics. The observed n value1.391 for drug release for F3G2 bespeak Super case II transport may be the result of sorption of the drug from the surface of NLC that is controlled by stress-induced relaxation which occurs at the boundary of the swollen shell. Conclusion: In vitro characterization of ACT (Acitretin) loaded NLC supports the objective that NLC can serve as a potential carrier for topical delivery of ACT and can also reduce oral toxicity associated with drug after stringent evaluation in the near future.

Formulation by Design (FbD) approach to develop pharmaceutically amended Diclofenac Sodium hydrogel as compared to marketed gel

The aim of the present study was to develop pharmaceutically better performing Diclofenac Sodium hydrogel through FbD approaches as compared to marketed gel. The quality target product profile was set for the critical quality attributes of the gel. The key material variables like Carbopol 934P, propylene glycol and Triethanolamine (TEA) were optimized using design of experiments. A response surface central composite design was used considering viscosity, pH and cumulative percentage permeation of the drug up to 120 min as responses. TEA had a significant effect on the pH at concentrations of 0.3182-3.6818% (w/w). The applicability of the optimized formulations was influenced by both Carbopol 934P (0.6591-2.3409%; w/w) and propylene glycol (PG; 6.591-23.409%; w/w) content due to their ability to alter the formulation viscosity. The optimized formulation, determined mathematically, contained 1.5% (w/w) Carbopol 934P. 2.0% (w/w) TEA and 15% (w/w) PG. The optimized hydrogel and marketed gel were evaluated for viscosity, spreadability, skin irritation, homogeneity and grittiness, texture analysis, in vitro release and ex vivo permeation studies. When these evaluation parameters were compared with a marketed gel in respect of all the evaluating tests, the optimized hydrogel was found to be far better formulation than the marketed one.

Formulation and Characterization of Eplerenone Mucoadhesive Buccal Tablets

Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.

Berberine Chloride Dihydrate Enthused Nanovesicles for the Management of Dermatitis Nanovesicles for Dermatitis

Background: Dermatitis is a common inflammatory skin disease that is affecting up to 25% of children and 1%-3% of adults worldwide. The paucity of the exact cure for dermatitis and untoward side effects of topical immunosuppressive steroids, has resulted in a great need for making use of complementary medicine to treat dermatitis. Objective: The present research work involved the development of Berberine chloride dihydrate (BCD) enthused nanovesicles i.e. ethosomes for the management of dermatitis. Method: Ethosomes were prepared by slight modification of cold method using varying concentrations of SPC (1-3%) and ethanol (10-40%) Optimized batch BCD 12 was further added to Carbopol 934P for gel formation. GEL BCD 12 was subjected to “anti-bacterial, dermatitis and skin irritation study. Result: The vesicles were in size range 142.42-398.31 nm while polydispersity index (PDI) ranges from 0.114-1.56 and for zeta potential it was from-18.8 to -39.4. Entrapment efficiency was from 46.05-88.79 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin upto 110 µm which was significantly higher than rhodamine solution (10 µm). In the anti-bacterial study, BCD loaded ethosomal gel (EG) showed maximum zone of inhibition of 18.5 mm against E. coli, 14.5 mm against P. aeruginosa and 23.0 mm against S. aureus. In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed marked decrease in amount of inflammatory cell nucleus in mice treated with BCD loaded ethosomal gel followed by 56% and 50 % increase in ear swelling and ear mass respectively in morphology study. Conventional marketed formulation showed nominal decrease in epidermal thickness, 66.67 % increase in ear thickness and 63.64 % increase in ear mass. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Conclusion: It can be concluded that ethosomal gel is not only an efficient carrier for BCD but also proves its potential for the management of dermatitis.

FORMULATION AND EVALUATION OF IN-SITU GEL CONTAINING LINEZOLID IN THE TREATMENT OF PERIODONTITIS

Objective: The intent to prepare and evaluate Linezolid in-situ gel in the treatment of periodontitis.
 Methods: pH-sensitive in-situ gel was formed by the cold method using a varying concentration of the drug, carbopol 934P and hydroxypropyl methylcellulose (HPMC) and carbopol 934P and sodium carboxy methylcellulose (CMC) (1:1,1:1.5,1:2,1:2.5). An optimized batch was selected based on gelling time and gelling capacity. The prepared in-situ gels were evaluated for appearance, pH, gelling capacity, viscosity, in vitro release studies, rheological studies, and finally, was subjected to drug content estimation and antibacterial activity test.
 Results: FTIR study shows drug and physical mixture were compatible with each other. The rheology of formulated in-situ gel exhibited a pseudoplastic flow pattern. this may be because when polymer concentration was increased the prepared formulations become more viscous and in turn delayed the drug release and from the prepared formulation, LF4 and SF4 have polymer concentrations i. e, 0.9% carbopol and sodium CMC showed drug release up to 12 h. 
 Conclusion: When carbopol is appropriately mixed with other suitable polymers it forms an in-situ gel-forming system that was substantiated by the property to transform into stiff gels when the pH is increased. The in-situ gel was prepared using a combination of carbopol-HPMC and carbopol-Na CMC The formulations LF1 to SF4 showed high linearity (R2 = 0.490-0.682), indicating that the drug was released from the prepared in-situ gel by the diffusion-controlled mechanism. Thus, the formulation of batches LF4 and SF4 containing carbopol: HPMC and carbopol: NaCMC in 1:2 ratios were considered as optimum formulation based on optimum viscosity, gelling capacity and to extend the in vitro drug release.

Design of emulgel platforms for local propolis delivery: The influence of type and concentration of carbomer

Emulgel systems gelled by adding carbomer 934P (C934P) have shown suitable physicochemical characteristics for propolis delivery aiming the therapy of dermatological disorders. However, there are other types of carbomers toxicologically preferable with different and important physicochemical properties to be utilized in emulgel systems, such as Carbopol 974P (C974P) and Carbopol 971P (C971P). In this sense, this work investigated formulations of different carbomer types (C934P, C97P and C974P) and concentrations, according to a factorial design 32. The systems were evaluated as mechanical textural and rheological characteristics. The physical stability of formulations also enabled the selection of the best formulations, which were evaluated as in vitro drug delivery. The texture profile analysis showed that C934P and C974P, at 1% (w/w) concentration, were responsible for improved mechanical characteristics. These same formulations were the only ones that displayed stability against centrifugation and were selected to the other tests. When submitted to rheological analysis they showed non-Newtonian pseudoplastic behavior and were viscoelastic. Rheological and textural mechanical characteristics confirmed the influence of temperature, type, and concentration of carbomer in the systems. The incorporation of propolis increased the softness of systems, suggesting easy local administration. Thus, emulgels composed of C934P or C974P 1% (w/w) are promising systems for controlled release of propolis and are worthy of further studies.

Design and Characterization of Combinational Domperidone-Famotidine Floating Drug Delivery System - In vitro and In vivo studies

Introduction: The drawbacks assosiated with oral administration of drugscan be controlled or minimized by gastro retentive formulations that remain buoyant within the stomach for an extended time by providing prolonged gastric retention and releasethe drug in an exceedingly extended manner thereby improving bioavailability. The current research was to develop and optimize Domperidone and Famotidine floating tablets with extended release by Quality by Design approach.
 Method: Based on QTPP (Quality Target Product Profile), CQAs (Critical Quality Attributes)wereidentified. Risk analysis by the evaluation of formulation and process parameters showed that optimizing the levels of polymers could reduce high risk to achieve the target profile. A 23factor experimental design with midpoints was selected for statistical analysis and optimization.
 Results: HPMC K100 and Carbopol 934P had a positive effect while ethyl cellulose demonstrated a negative effect on the selected responses. Drug release kinetics followed the first-order release with Higuchi diffusion and Fickian diffusion. Optimized formula satisfying all the required parameters was selected and evaluated. The predicted response values were in close agreement with experimental response values. Abdominal X-ray imaging after oral administration of the tablets on a healthy rabbit’s stomach confirmed the extended floating behavior with shorter lag time. In vivo, pharmacokinetic studies in rabbits revealed that the optimized formulation exhibited prolonged drug release with enhanced Cmax, tmax, AUCo-t, and t1/2 of an optimized product when compared to the marketed product.
 Conclusions: It has been concluded that the application of Quality by Design in the formulation and optimization reduced the number of trials to produce a cost-effective formula.

Formulation and evaluation of transdermal nanogel for delivery of artemether.

Artemether (ART) is second to artesunate in being the most widely used derivatives of artemisinin in combination therapy of malaria. Nanostructured lipid carrier (NLC) formulations were prepared following our previous report using optimized ART concentration of 0.25g dissolved in 5% w/v mixture of solid (Gelucire 43/01 and Phospholipon 85G) and liquid (Transcutol) lipids at 90°C. An aqueous surfactant phase at 90°C was added (dropwise) under magnetic stirring (1000rpm) for 5min. The pre-emulsion was speedily homogenized at 28,000rpm for 15min and further probe sonicated at 60% amplitude (15min). Resultant sample was cooled at room temperature and frozen at -80°C prior to lyophilization. The freeze-dried sample was used for solid-state characterization as well as in the formulation of transdermal nanogels using three polymers (Carbopol 971P, Poloxamer 407, and Prosopis africana peel powder) to embed the ART-NLC, using ethanol as a penetration enhancer. Transdermal ART-nanogels were characterized accordingly (physical examination, pH, drug content, rheology, spreadability, stability, particle size and morphology, skin irritation, in vitro and ex vivo skin permeation, and analysis of permeation data), P < 0.05. Results indicated that ART nanogels showed good encapsulation, drug release, pH-dependent swelling, stability, and tolerability. Overall, ART nanogels prepared from Poloxamer 407 showed the most desirable drug permeation, pH, swellability, spreadability, viscosity, and transdermal antiplasmodial properties superior to PAPP-ANG > C971P-ANG. A two-patch/week concurrent application of the studied nanogels could offer 100% cure of malaria as a lower-dose (50mg ART) patient-friendly regimen devoid of the drug's many side effects.

Thermoresponsive Hydrogel-Loading Aluminum Chloride Phthalocyanine as a Drug Release Platform for Topical Administration in Photodynamic Therapy.

Phthalocyanine aluminum chloride (Pc) is a clinically viable photosensitizer (PS) to treat skin lesions worsened by microbial infections. However, this molecule presents a high self-aggregation tendency in the biological fluid, which is an in vivo direct administration obstacle. This study proposed the use of bioadhesive and thermoresponsive hydrogels comprising triblock-type Pluronic F127 and Carbopol 934P (FCarb) as drug delivery platforms of Pc (FCarbPc)-targeting topical administration. Carbopol 934P was used to increase the F127 hydrogel adhesion on the skin. Rheological analyses showed that the Pc presented a low effect on the hydrogel matrix, changing the gelation temperature from 27.2 ± 0.1 to 28.5 ± 0.9 °C once the Pc concentration increases from zero to 1 mmol L-1. The dermatological platform showed matrix erosion effects with the release of loaded Pc micelles. The permeation studies showed the excellent potential of the FCarb platform, which allowed the partition of the PS into deeper layers of the skin. The applicability of this dermatological platform in photodynamic therapy was evaluated by the generation of reactive species which was demonstrated by chemical photodynamic efficiency assays. The low effect on cell viability and proliferation in the dark was demonstrated by in vitro assays using L929 fibroblasts. The FCarbPc fostered the inhibition of Staphylococcus aureus strain, therefore demonstrating the platform's potential in the treatment of dermatological infections of microbial nature.

Investigation of the physicochemical stability of emulgels composed of poloxamer 407 and different oil phases using the Quality by Design approach

Emulgels can be prepared easily and provide the efficient drug release of hydrophilic and hydrophobic drugs. In this work, emulgel systems containing poloxamer 407, Carbopol 974P® or polycarbophil, sesame oil or isopropyl myristate were prepared using Quality by Design and the physicochemical damages were investigated regarding the preliminary stability studies. The physicochemical stability was assessed according to six freeze-thaw cycles, where the appearance, phase separation (fracture), droplet size and instability index were determined. The stable formulations were further characterized by sol-gel transition temperature. The freeze-thaw cycles and analytical centrifuging showed consistent and complementary results evidencing that lower concentration of bioadhesive polymers fostered the phase separation. Formulations showed to be polydisperse systems with droplet size dependent of the freeze-thaw cycles. The stable systems were selected by Quality by Design approach, and they showed suitable gelation temperature for future pharmaceutical and biomedical applications.

Enhancement of Transdermal Permeation of Indinavir Sulfate via EthosomeVesicles

The aim of the present study is to investigate the potential of ethosomal formulations for transdermal delivery of indinavir sulphate from ethosomes. Vesicles containing phosphatidylcholine mixed with ethanol and indinavir sulphate were prepared by conventional mechanical stirrer method and characterized by various parameters (vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity and in vitro drug release). The effect of different formulation variable on skin permeation of indinavir sulphate was studied via synthetic semipermeable membrane or skin of new born mice by using diffusion cell. The selected system were incorporated into carbopol 934P gel and evaluated for both drug permeation and mice skin deposition. The optimized ethosomal formulation showed transdermal flux of 25.01±0.34 μg/cm2 /h across rat skin as compared to 2.98±0.21μg/cm2 /h for plane drug solution, 4.28±0.54 μg/cm2 /h for hydroethanolic solution and 9.7±0/21 μg/cm2 /h for classical liposomes. The obtained flux was nearly 7.5 and 12.04 times higher than conventional liposomal formulation bearing indinavir sulphate and plain drug solution. These results suggest that ethosomes are potential vehicles for improved transdermal delivery of indinavir sulphate.

Formulation Development and Evaluation of Gastro Retentive Matrix Tablet of Levamisole Hydrochloride

The aim of current study was to develop suitable gastroretentive tablet of Levamisole HCl for prolonging the retention of Levamisole in stomach. Floating tablets were prepared by using HPMC K4M and Carbopol 934p in combination and their effect on floating, swelling and release of Levamisole HCl was studied. Optimization of drug release were carried out by taking different concentration of HPMC K4M and Carbopol 934p. It was found that HPMC and Carbopol with concentration 35% and 22% in tablet give satisfactory release and batch was selected for 32 factorial design. In this study all the formulation were subjected to physical evaluation parameter such as Hardness, Friability, content uniformity all were found to be within limits. In-vivo study F5 formulation was carried out to check the buoyancy of tablet. Tablet float in stomach of rabbit for 8 hours without adhering to gastric mucous. Stability studies of F5 formulation indicated that formulation is stable for 3 months at 40o C and 75% RH. The formulation retained its integrity and In-vitro performance.

MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION

Objective: The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release.&#x0D; Methods: Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, in vitro drug release and ex vivo permeation through porcine buccal mucosa.&#x0D; Results: Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and in vitro drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower in vitro drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of ex vivo permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period.&#x0D; Conclusion: Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability.

Formulation and evaluation of nano structured lipid carriers for intranasal delivery of Buspirone hydrochloride

The aim of this work was to formulate buspirone hydrochloride (BH) NLCs for intranasal administration to improve BH bioavailability. The BH loaded NLCs were prepared by hot high-pressure homogenization technique using Precirol ATO 5, olive oil and tween 80 as solid lipid, liquid lipid and surfactant, respectively. Carbopol 934P and HPMC K4M were used to convert NLCs dispersion into NLCs based in-situ nasal gelling solution to improve its mucoadhesive property for intranasal administration. A factorial design approach was used to study the effect of independent variable (amount of Precirol ATO 5 and olive oil) on the dependent variables (particle size and percentage entrapment efficiency (%EE). The optimized formulation was characterized for particle size, zeta potential, %EE, and surface morphology. Fourier transform infrared (FTIR) spectroscopy was used to study the possible BH-lipid complex formation. Further, viscosity determination, stability studies, in-vitro drug release, ex-vivo skin permeation studies and ex-vivo nasal toxicity studies of BH loaded NLCs nasal gelling solution were carried out. The BH loaded NLCs (batch F8) showed particle size of 111.8nm, %EE of 78.34% and zeta potential of-44.3mV. Scanning electron microscopy (SEM) confirmed spherical shape of NLCs. In vitro drug release and ex vivo skin permeation studies of BH loaded NLCs and BH loaded NLCs in-situ nasal gelling solution showed 71.26% drug permeation.

Nose-to-brain delivery of teriflunomide-loaded lipid-based carbopol-gellan gum nanogel for glioma: Pharmacological and in vitro cytotoxicity studies

The research work was intended to formulate teriflunomide (TFM) loaded nano lipid-based (TNLC) carbopol-gellan gum in situ gel (TNLCGHG) and to investigate its therapeutic efficacy against glioma, a brain and spine tumor. Nanoformulation was developed using gellan gum and carbopol 974P as gelling and mucoadhesive agents, respectively, Glyceryl di-behenate and Glyceryl mono-linoleate blend as lipids, and Gelucire 44/14: water blend as surfactant system. Globule size, PDI, zeta potential, encapsulation efficiency, mucoadhesive strength, and nasal permeation were found to be 117.80 nm, 0.56, −21.86 mV, 81.16%, 4.80 g, and 904 μg/cm2, respectively. Anticancer efficacy of TFM-loaded nano lipid-based carbopol-gellan gum in situ gel (TNLCGHG) was determined in human U-87MG glioma cell line. IC50 was found 7.0 μg/mL for TNLCGHG, 4.8 μg/mL for pure TFM, and 78.5 μg/mL for TNLC, which approve the superiority of surfactant along with gellan gum as permeation enhancer. Brain Cmax for technetium (99mTC) labeled intranasal (i.n.) 99mTC-TNLCGHG was found 2-folds higher than 99mTC-TNLC (i.n.) and 99mTC-TNLC intravenous (i.v.) because the TNLCGHG formulation contains surfactant with natural gelling polymers, which promisingly improved drug permeability. Finally, this research revealed encouraging outcomes and successfully developed intranasal TNLCGHG nanoformulation as a novel tool for safe delivery of TFM in glioma patients.