Mucoadhesive Force Research Articles

Caspofungin formulations for buccal and sublingual mucosae anti-fungal infections: physicochemical characterization, rheological analysis, release and ex vivo permeability profiles

Aim Oral candidiasis is often challenging due to limited effectiveness of topical treatments. This study aimed to develop novel caspofungin formulations for administration onto the oral mucosa to enhance drug retention and efficacy. Method Five caspofungin (2%, w/v) formulations were developed to assess their permeability, retention and mucoadhesiveness. Ex vivo permeability assays were performed on buccal and sublingual mucosae, and histological analyses conducted to evaluate tissue tolerance. Results Formulation composed of chitosan demonstrated the highest retention in both buccal (5183.24 ± 587.32 µg/cm2) and sublingual (1090.72 ± 110.26 µg/cm2) mucosae. Other formulations exhibited significantly lower retention, ranging from 7.53 ± 0.81 to 1852.10 ± 193.24 µg/cm2 in buccal mucosa and 1.64 ± 0.14 to 317.74 ± 31.78 µg/cm2 in sublingual mucosa. Chitosan-based formulation exhibited the highest mucoadhesive strength, with values of 5179.05 ± 31.99 mN/cm2 for buccal and 7026.10 ± 123.41 mN/cm2 for sublingual mucosae, and also superior extensibility, which facilitates application in the oral cavity. All formulations showed antifungal activity against Candida spp., and histological analyses revealed minor epithelial alterations. Conclusion The developed formulations offer distinct advantages for treating oral candidiasis, with chitosan formulation emerging as the most promising due to its superior retention, mucoadhesion force, and spreadability, making it a potential candidate for further clinical investigation.

Effect of Pluronic F127 Concentration on Gelling Temperature and other Parameters of Lomustine Mucoadhesive In-Situ Gel

Pluronic F127 is one of the widely used thermoreversible gelling agent, and used in sol-to-gel transformation. It has been used to localize drug delivery such as nose-to-brain delivery which allows the direct targeting of drug molecules bypassing the systemic effect and BBB (Blood Brain Barrier). The anticancer drug lomustine had poor oral bioavailability in addition to its serious side effect, therefore, developing more effective drug delivery with direct targeting towards the brain through intra-nasal administration applying nanoemulsion-based-in situ gel technology is a promising alternative. The work involved formulation of lomustine as in situ gel using Pluronic F127 and study the effect of the polymer on solution to gel transition temperature, gelation behaviour, spreadability, mucoadhesive force, residence time and residence drug percentage, as well as in vitro drug release. The results showed acceptable pH and high drug content, beside increased Pluronic percentage (from 15 to 20%) led to reduced gelation temperature from 33°C to 27°C and spreadability, improved gelling properties from + to +++, increasing mucoadhesive force from 4965.33 to 9866.30 dyne/cm2 as well as prolonged residence time from 30 to 66 min and in vitro drug release where was 120 min for 100% drug release from F1 that contained 15% of the polymer to 210 min for F3 with 20% polymer. Therefore, modifying the Pluronic F127 percent in the in situ formulas could optimize the required formula for targeting the anticancer to treat brain cancer via nose-to-brain delivery.

Optimization and comparison of unidirectional lidocaine-loaded buccal patch with the articaine-loaded buccal patch to reduce injection pain and increment of patients' compliance in dental procedures: A double‐blind randomized controlled trial

IntroductionNervous patients often postpone dental visits until they are in severe pain, exacerbating anxiety. Buccal patches provide a noninvasive method of delivering drugs between the upper gum and cheek, offering local and systemic effects. Prior research has demonstrated the effectiveness, safety, and reliability of topical lidocaine or articaine patches for oral anesthesia. Consequently, this study aimed to develop a three-layered buccal drug delivery system for topical anesthetics. MethodsThe first step was preparing and optimizing lidocaine-loaded three-layer patches using Design-expert software. The effects of ethylcellulose, Eudragit, and carbopol concentrations were investigated on patch characteristics, including mucoadhesion, Young's modulus, and Elongation-at-break. Subsequently, patches were fabricated according to the optimized formulation determined by the software, and their efficacy was studied in a randomized, double-blind clinical trial. Participants received either lidocaine or articaine-loaded compared with placebo in a split-mouth study. They evaluated their pain levels using the Visual Analogue Scale (VAS), and the onset and duration of action were recorded for each treatment. ResultsAccording to the results, increasing ethyl cellulose and Eudragit concentrations improved mucoadhesion force (p < 0.05) while increasing ethyl cellulose and reducing Eudragit concentrations increased Young's modulus (p < 0.05). Increasing Carbopol and decreasing Eudragit concentrations also raised elongation at break significantly in the patch (p < 0.05). Treatment with lidocaine-loaded patches resulted in lower VAS scores and faster onset of action in patients than articaine-loaded patches. However, the duration of the effect was longer in the former(p < 0.001). ConclusionBased on the responses' analysis, the formulation of the 3-layered buccal patch was optimized. This formulation comprised 4.72 % ethyl cellulose, 2 % Carbopol, and 5 % eudragit. Clinical evaluation results showed that loading the optimized formulation with lidocaine was more efficient in controlling the injection pain than articaine. Trial registrationThis trial was prospectively registered with irct.behdasht.gov.ir (registration number: IRCT20210118050067N2) on Aug 19, 2022.

Formulation and Evaluation of Bilastine Thermosensitive Mucoadhesive Ophthalmic in situ Gel

Background: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparent, having a pH ranging from 7.4 to 7.5 and a gelation temperature between 29.5 and 34.7 °C. Increasing the concentrations of P-407 and HPMC increased viscosity, gel strength, and mucoadhesion force, but caused a decrease in gelation temperature and drug release. Formula (F 14) containing P 407/P 188/HPMC as 19/4/0.75% w/v, respectively, exhibited favorable characteristics, including optimal gelation temperature (33°C), drug content (93%), gel strength (40 sec), mucoadhesive force (6125 dyne/cm2), and 91.4% in vitro drug release over 5 hours. Conclusions: The bilastine mucoadhesive in situ gel formulation is presented as a promising ophthalmic formulation for the treatment of allergic conjunctivitis.

Analysis of Key Factors for Evaluating Mucosal Adhesion Using Swine Buccal Tissue

The assessment of the mucoadhesive properties peak mucoadhesive force (Fmax) and work of mucoadhesion (Wmuc) with texture analyzers is a common in vitro method for analyzing formulation capabilities. Challenges arise in selecting and standardizing experimental conditions due to various variables influencing mucoadhesion. This complexity hampers direct product performance comparisons. In our study, we explored factors (contact force and time, probe speed and mucin in artificial saliva) impacting a model formulation's mucoadhesive capacity. Using Omcilon-A®Orabase on porcine buccal mucosa, we systematically varied experimental conditions, employing a statistical approach (Central Composite Design - CCD). Three variables (contact force, contact time, probe speed) and their interactions were assessed for their impact on Fmax and Wmuc. Results showed that contact time and force positively affected Fmax, while only contact time influenced Wmuc. In the mucin artificial saliva test, a force of 0.5 N, time of 600 s, and speed of 1 mm/s yielded optimal Fmax (0.587 N) and Wmuc (0.468 N.s). These conditions serve as a reference for comparing mucoadhesive properties of formulations for topical oral use.

Algae-Based Nanoparticles for Oral Drug Delivery Systems.

Drug administration by oral delivery is the preferred route, regardless of some remaining challenges, such as short resident time and toxicity issues. One strategy to overcome these barriers is utilizing mucoadhesive vectors that can increase intestinal resident time and systemic uptake. In this study, biomimetic nanoparticles (NPs) were produced from 14 types of edible algae and evaluated for usage as oral DDSs by measuring their size, surface charge, morphology, encapsulation efficiency, mucoadhesion force, and cellular uptake into Caco-2 cells. The NPs composed of algal materials (aNPs) exhibited a spherical morphology with a size range of 126-606 nm and a surface charge of -9 to -38 mV. The mucoadhesive forces tested ex vivo against mice, pigs, and sheep intestines revealed significant variation between algae and animal models. Notably, Arthospira platensis (i.e., Spirulina) NPs (126 ± 2 nm, -38 ± 3 mV) consistently exhibited the highest mucoadhesive forces (up to 3127 ± 272 µN/mm²). Moreover, a correlation was found between high mucoadhesive force and high cellular uptake into Caco-2 cells, further supporting the potential of aNPs by indicating their ability to facilitate drug absorption into the human intestinal epithelium. The results presented herein serve as a proof of concept for the possibility of aNPs as oral drug delivery vehicles.

FORMULATION AND DEVELOPMENT OF BIOADHESIVE PELLETS FOR MANAGEMENT OF HELICOBACTER PYLORI INFECTION

Helicobacter pylori, a gram-negative bacterium, is a group I carcinogen which is responsible for duodenal ulcer, gastric ulcer, and gastric cancer. The existing treatment is based on the use of proton pump inhibitors, but is inadequate owing to factors such as low concentration of drug reaching the target site, short residence time, and resistance to activity. Intending to mitigate these limitations, bioadhesive pellets of tinidazole and pantoprazole sodium sesquihydrate for the management of H. pylori infection were developed. Tinidazole-loaded pellets will act on gastric mucosa and pantoprazole-loaded pellets will release the drug in the intestine. Readily dispersible bioadhesive pellets were formulated by extrusion spheronization using Noveon® AA and hydroxypropyl methyl cellulose (HPMC) as the matrix-forming polymers and microcrystalline cellulose as the core-forming agent. The size of placebo pellets was 1.192±0.017mm. Pantoprazole pellets were coated with Eudragit® S100 to achieve sustained drug release in the intestine. In vitro release studies of pellets showed that 98.331±0.456% and 99.438±0.465% of tinidazole and pantoprazole, respectively were released by the end of 8 h. Ex vivo mucoadhesion study on the gastric mucosa of goat demonstrated a mucoadhesive force of 2.3544±0.02 N. The study thus indicates that the developed formulation sustains the release of tinidazole as well as pantoprazole sodium and could prove to be efficacious and promising for H. pylori eradication at lower doses, reduced adverse effects, and enhanced bioavailability.

Formulation development and evaluation of nasal in situ gel of promethazine hydrochloride

Objective The present work aims to develop mucoadhesive thermosensitive nasal in situ gel for Promethazine hydrochloride using quality by design (QbD) approach. It can reduce nasal mucociliary clearance (MCC) and increase residence of the drug on nasal mucosa. This might increase drug absorption to improve bioavailability of the drug as compared to oral dosage form. Significance Promethazine hydrochloride is an antiemetic drug administered by oral, parenteral and rectal routes. These routes have poor patient compliance or low bioavailability. Nasal route is a better alternative as it has large surface area, high drug absorption rate and no first pass effect. Its only limitation is short drug retention time due to MCC. By formulating a mucoadhesive in situ gel, the MCC can be reduced, and drug absorption will be prolonged. Thus, improving bioavailability. Method In-situ gel was prepared by cold method having material attributes as concentration of Poloxamer 407 (X1) as gelling agent and hydroxypropyl methyl cellulose K4M (X2) as mucoadhesive agent. Critical Quality Attributes (CQA) were gelation temperature, mucoadhesive force and ex-vivo diffusion. Central composite design (CCD) was adopted for optimization. Result Optimized formulation satisfied all the CQA significant for nasal administration. Moreover, the formulation was found to be stable in accelerated stability studies for 3 months. Conclusion It can be concluded that since the drug can easily permeate through nasal mucosa and can gain access directly in the brain without undergoing first pass metabolism along with increased residence due to mucoadhesion, mucoadhesive in situ gel has potential to increase drug bioavailability.

Development of Carvedilol Nanoformulation-Loaded Poloxamer-Based In Situ Gel for the Management of Glaucoma.

The objective of the current study was to fabricate a thermosensitive in situ gelling system for the ocular delivery of carvedilol-loaded spanlastics (CRV-SPLs). In situ gel formulations were prepared using poloxamer analogs by a cold method and was further laden with carvedilol-loaded spanlastics to boost the precorneal retention of the drug. The gelation capacity, rheological characteristics, muco-adhesion force and in vitro release of various in situ gel formulations (CS-ISGs) were studied. The optimized formula (F2) obtained at 22% w/v poloxamer 407 and 5% w/v poloxamer 188 was found to have good gelation capacity at body temperature with acceptable muco-adhesion properties, appropriate viscosity at 25 °C that would ease its ocular application, and relatively higher viscosity at 37 °C that promoted prolonged ocular residence of the formulation post eye instillation and displayed a sustained in vitro drug release pattern. Ex vivo transcorneal penetration studies through excised rabbit cornea revealed that F2 elicited a remarkable (p ˂ 0.05) improvement in CRV apparent permeation coefficient (Papp = 6.39 × 10-6 cm/s) compared to plain carvedilol-loaded in situ gel (CRV-ISG; Papp = 2.67 × 10-6 cm/s). Most importantly, in normal rabbits, the optimized formula (F2) resulted in a sustained intraocular pressure reduction and a significant enhancement in the ocular bioavailability of carvedilol, as manifested by a 2-fold increase in the AUC0-6h of CRV in the aqueous humor, compared to plain CRV-ISG formulation. To sum up, the developed thermosensitive in situ gelling system might represent a plausible carrier for ophthalmic drug delivery for better management of glaucoma.

Development of an Antiviral Ion-Activated In Situ Gel Containing 18β-Glycyrrhetinic Acid: A Promising Alternative against Respiratory Syncytial Virus.

The human respiratory syncytial virus (hRSV) is a major cause of serious lower respiratory infections and poses a considerable risk to public health globally. Only a few treatments are currently used to treat RSV infections, and there is no RSV vaccination. Therefore, the need for clinically applicable, affordable, and safe RSV prevention and treatment solutions is urgent. In this study, an ion-activated in situ gelling formulation containing the broad-spectrum antiviral 18β-glycyrrhetinic acid (GA) was developed for its antiviral effect on RSV. In this context, pH, mechanical characteristics, ex vivo mucoadhesive strength, in vitro drug release pattern, sprayability, drug content, and stability were all examined. Rheological characteristics were also tested using in vitro gelation capacity and rheological synergism tests. Finally, the cytotoxic and antiviral activities of the optimized in situ gelling formulation on RSV cultured in the human laryngeal epidermoid carcinoma (HEp-2) cell line were evaluated. In conclusion, the optimized formulation prepared with a combination of 0.5% w/w gellan gum and 0.5% w/w sodium carboxymethylcellulose demonstrated good gelation capacity and sprayability (weight deviation between the first day of the experiment (T0) and the last day of the experiment (T14) was 0.34%), desired rheological synergism (mucoadhesive force (Fb): 9.53 Pa), mechanical characteristics (adhesiveness: 0.300 ± 0.05 mJ), ex vivo bioadhesion force (19.67 ± 1.90 g), drug content uniformity (RSD%: 0.494), and sustained drug release over a period of 6 h (24.56% ± 0.49). The optimized formulation demonstrated strong anti-hRSV activity (simultaneous half maximal effective concentration (EC50) = 0.05 µg/mL; selectivity index (SI) = 306; pre-infection EC50 = 0.154 µg/mL; SI = 100), which was significantly higher than that of ribavirin (EC50 = 4.189 µg/mL; SI = 28) used as a positive control against hRSV, according to the results of the antiviral activity test. In conclusion, this study showed that nasal in situ gelling spray can prevent viral infection and replication by directly inhibiting viral entry or modulating viral replication.

Design and Development of Sertaconazole Nitrate Loaded Silver Nanoparticulate Mucoadhesive Tablets for the Treatment of Vaginal Candidiasis

Vaginal candidiasis, a fungal infection estimates that 75 % of women will be suffering at least once during their lifetime. The disorders of this infection might be premature birth, pelvic inflammation, abortion, the transmission of sexual disorders, etc. In the present research, mucoadhesive vaginal tablets containing sertaconazole nitrate-loaded silver nanoparticles formulations were developed which increases the proximity period of the medicine with the vaginal mucosa, showing sustained drug release. The drug-loaded silver nanoparticle was synthesized by the chemical reduction method. There was successful conjugation of sertaconazole nitrate with silver nanoparticles (Ser-AgNP1) therefore, the drug’s solubility is increased by 2.51 folds. The confirmation of silver nanoparticles was accessed by UV-visible spectroscopy. The mucoadhesive vaginal tablets were formulated and evaluated for swelling index, mucoadhesive force, residence time, In vitro dissolution and release kinetics, stability, and antifungal study. Optimized batch F8 was selected based on optimum mucoadhesive force (2.59±0.25N), % swelling index (86.50±0.11%), and sustained drug release (95.63±0.16%) up to 12 hr and showed greater antifungal activity. Overall study reveals that a prepared novel formulation, a mucoadhesive vaginal tablet containing sertaconazole nitrate loaded silver nanoparticles prevail over sertaconazole nitrate poor solubility and delivered drug during an extended period of time and also improved antifungal activity against Candida albicans.

Development of Mucoadhesive Chitosan-Iodoacetamide Buccal Tablets for Local Delivery of Dextromethorphan

Abstract This study aimed to synthesize a chitosan (CHI) derivative, chitosan-iodoacetamide (CHI-IA), with enhanced mucoadhesive properties and develop buccal mucoadhesive tablets of CHI-IA for local delivery of dextromethorphan (DXT). Mucoadhesive CHI-IA was synthesized by a chemical reaction between CHI and iodoacetic acid (IA) in different weight ratios. The synthesized CHI-IA was characterized by Fourier-transformed infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR) to confirm the chemical structure and assure successful synthesis. DXT was selected as the model drug to be incorporated into the matrix tablet to develop mucoadhesive buccal cough relief tablets. The mucoadhesive strength of the CHI-IA tablets was determined by a texture analyzer. Moreover, the drug content and the release characteristics of DXT from the mucoadhesive tablets were evaluated. The FT-IR and NMR spectra of CHI-IA indicated the conjugation of IA on the structure of CHI. The CHI-IA tablets exhibited a 4-time increase in mucoadhesion force compared with that of unmodified CHI. Moreover, a gradual release of DXT from the tablets was observed, and the release kinetics best fit with the Higuchi model (R2 = 0.9912). Therefore, the CHI-IA could be applied as the mucoadhesive carrier system for drug delivery. Keywords: Chitosan, Iodoacetic acid, Mucoadhesive, Buccal tablets, Dextromethorphan

Mucoadhesive Films of Liquorice and Chlorhexidine Gluconate for Treating Mouth Ulcers

Abstract: Objectives: Mouth ulcer is a rupture or breaks in the oral mucosal membrane and it leads to atrophy and ulcers in the oral cavity. It increases the risk of infections with the Candida species Inherited trauma and aphthous stomatitis, a disorder characterised by the recurrent production of oral ulcers for unknown reasons, are the most common causes of oral ulceration. Study Design: This study aimed to develop two separates buccal mucoadhesive films, using model drug deglycyrrhizinated liquorice and chlorhexidine gluconate. The film was assessed for weight, thickness, pH, folding endurance, swelling index, mucoadhesive force, % moisture content, drug uniformity, in vitro release of drug, anti-microbial effect including anti-inflammatory activity and scanning electron microscopy. The developed formulations we re-evaluated for surface pH, folding endurance, swelling index, mucoadhesive force, and percentage moisture loss. Results and Conclusion: The results showed that the developed oral films were having good anti-inflammatory activity with an anti-microbial effect. Keywords: Deglycyrrhizinated liquorice, Chlorhexidine gluconate, Mucoadhesive buccal films, Anti-inflammatory activity.

Rectal Administration of Celecoxib Liquid Suppositories with Enhanced Bioavailability and Safety in Rats.

Celecoxib is generally used for the treatment of rheumatoid arthritis, however its poor bioavailability and cytotoxicity in pure form have reduced its therapeutic efficacy. This study aims to develop celecoxib liquid suppositories with improved bioavailability and reduced toxicity. The celecoxib liquid suppositories were prepared by thoroughly mixing celecoxib, poloxamer 188 and poloxamer 407, and tween-20, respectively used as drug, polymers and surfactant, in triple distilled water using cold technique. The developed liquid suppositories were characterized in terms of their gelation temperature, gelation time, and gel strength. Moreover, the muco-adhesive force was determined for the suppositories. The release behavior of the liquid suppositories was investigated in distilled water and compared with drug suspension. Furthermore, pharmacokinetics and morphological studies were carried out in rats after rectal administration of the celecoxib liquid suppository compared with drug suspension. Poloxamer 188 and Tween-20 concentrations have significantly reduced the gelation temperature and time; however, the gel strength and bio-adhesive force were significantly enhanced. The concentration of celecoxib has no significant effect on the properties of liquid suppositories. A significantly enhanced and potentially sustained drug release was observed from the celecoxib liquid suppositories as compared with the drug suspension. The optimized formulation was easy to administer rectally because it quickly forms gel upon insertion into the body due to a suitable gelation temperature of about 31.7 °C. After rectal administration in rats, the celecoxib liquid suppository gave a significantly increased pharmacokinetic profile including enhanced plasma concentration and 9.7 fold improved area under the curve (AUC) compared to the drug suspension. Additionally, the morphology study exhibited no toxicity to the rectal tissue, no signs of irritation, or injury after the application of suppository. However, severe rectal tissue toxicity and irritation was observed in the suspension treated rectum. It can be concluded that the liquid suppository system may significantly enhance the solubilization and bio-availability of sparingly water-soluble drugs as evident in the case of celecoxib with no toxicity at the site of application.

Assessment of Mucoadhesion Potential of Thiolated Pectin Extracted from Citrus limon

Abstract: Aim: This study aimed to extract pectin from Citrus limon, synthesize thiolated pectin (TFP), and assess its mucoadhesion capability utilizing in-vitro and ex-vivo methodologies. Materials and Methods: Wilhelmy`s approach, the falling sphere method, the modified physical balancing method, and others were used to measure the mucoadhesion force of pectin and TFP and compared with chitosan (CS) and sodium carboxymethylcellulose (SCMC). Results: FTIR spectra containing carboxyl and hydroxyl groups confirmed that pectin formed a hydrogen connection with the mucosa. The outcome demonstrates that, under the experimental setup utilized in this study, pectin’s mucoadhesive qualities were equivalent to CS but less so than SCMC. The ability of the bulk of these polymers to adhere to one another is dependent on non-covalent chemical connections such as hydrogen bonds, ionic contacts, and van der Waals forces, amongst other types of interactions. Since these interactions are not as strong as covalent connections, localization of dosage forms cannot be guaranteed. To confirm the enhanced mucoadhesion potential of pectin through the thiolation procedure, pectin was thiolated and TFP was assessed for mucoadhesion potential using the same methodologies. Conclusion: In nutshell, pectin has good mucoadhesion properties, but to use pectin in mucoadhesion drug delivery systems, it is necessary to increase pectin’s mucoadhesion potential through appropriate methods like thiolation, etc. Keywords: Mucoadhesion, Pectin, Thiolation, Chitosan, Sodium Carboxymethylcellulose.

Development and Evaluation of Sodium Alginate/Carbopol 934P-Co-Poly (Methacrylate) Hydrogels for Localized Drug Delivery.

This research was carried out to create a pH-responsive polymeric system for the targeted drug delivery of Diloxanide furoate. It relied on sodium alginate (Na-Alg) and Carbopol 934P as building blocks. Using an aqueous free radical polymerization method, SCH1-SCH12 was created with varying polymer, MAA, and MBA input ratios. Positive outcomes were seen in the swelling and release profiles at higher pH levels. Hydrogel formation, as well as component compatibility, thermal stability, and Diloxanide furoate loading, were all validated by instrumental characterization. A drug loading percentage of 83.56% was determined, with the swelling reaching 743.19%. For the formulation with MBA, the gel fraction was 94.58%. The release of diloxanide furoate increased to 91.77% at neutral pH. The formulation containing Carbopol 934P provided the highest mucoadhesion force (3993.42 dynes/cm2). The created hydrogel has been shown to be biocompatible by toxicological testing of the network. Based on the findings, the created polymeric nexus proved promising for pH-dependent localized and regulated delivery of Diloxanide furoate.

Use of factorial design in formulation and evaluation of intrarectal in situ gel of sumatriptan.

The study's goal was to create an in situ intrarectal mucoadhesive gel of sumatriptan (SMT) combining mucoadhesive polymer (xyloglucan) and thermosensitive polymers (poloxamer 407 and poloxamer 188) to prolong rectal residence time for treatment of migraines. Nine SMT mucoadhesive rectal in situ gel (RIG) formulas were created by mixing poloxamer 407 (18%, 19%, or 20%) with poloxamer 188 (5%), a mucoadhesive polymer at various doses (0.1, 0.2, and 0.3) as well as SMT (25 mg/ml). The prepared suppositories underwent for mucoadhesive force, gelation temperature, and gelation time. When SMT and mucoadhesive polymer were added to the poloxamer mixture, the gelation temperature dropped; however, poloxamer 188 had the opposite effect. These polymers supported the prepared liquids' ability to adhere to mucous membranes and form a strong gel. The transition gelation temperature of the poloxamer solution rose as a result of the addition of poloxamer 188. The findings showed that the formula RIG5 which is composed of poloxamer 407 (19%), poloxamer 188 (5%), and xyloglucan (0.2%) had an ideal transition temperature of 36.33°C, gel strength of 44.66°C, mucoadhesive force of 6409°C, and in vitro drug release of 93.98% over an 8-hour period. In light of this, it can be said that SMT was successfully manufactured as RIG without causing any chemical reaction with its additives.

Formulation and characterization of lamotrigine nasal insert targeted brain for enhanced epilepsy treatment

Lamotrigine. (LMT) is a triazine drug has an antiepileptic effect but with low water solubility, dissolution rate and thus therapeutic effect. Spanlastics are nano-vesicular carriers’ act as site-specific drug delivery system. Intranasal route could direct the drug from nose to brain and provide a faster and more specific therapeutic effect. Therefore, this study aimed to upload lamotrigine onto nano-vesicles using spanlastic nasal insert delivery for effective epilepsy treatment via overcoming lamotrigine’s low solubility and improving its bioavailability. Lamtrigine-loaded nano-spanlastic vesicles were prepared by ethanol injection method. To study different formulation factor’s effect on formulations characters; particle size (PS), Zeta potential (ZP), polydispersity index (PDI), entrapment efficiency percentage (EE%) and LMT released amount after 6 h (Q6h); 2^1 and 3^1 full factorial designs were employed. Optimized formula was loaded in lyophilized nasal inserts formulation which were characterized for LMT release and mucoadhesion. Pharmacokinetics studies in plasma and brain were performed on rats to investigate drug targeting efficiency. The optimal nano-spanlastic formulation (F4; containing equal Span 60 amount (100 mg) and edge activator; Tween 80) exhibited nano PS (174.2 nm), high EE% (92.75%), and Q6h > 80%. The prepared nasal inserts (S4) containing 100 mg HPMC has a higher mucoadhesive force (9319.5 dyne/cm2) and dissolution rate (> 80% within 10 min) for rapid in vivo bio-distribution. In vivo studies showed considerable improvement brain and plasma’s rate and extent absorption after intranasal administration indicating a high brain targeting efficiency. The results achieved indicate that nano-spanlastic nasal-inserts offer a promising LMT brain targeting in order to maximize its antiepileptic effect.

Preparation and in-vitro Evaluation of Secnidazole as Periodontal In-situ Gel for Treatment of Periodontal Disease

This study aims to develop a thermosensitive mucoadhesive periodontal in situ gel of secnidazole for local release of drug for treatment of periodontitis, in order to increase the drug residence time and to increase patient compliance while lowering the side effects of the drug. Cold method was used to prepare 30 formulas of secnidazole periodontal in situ gel, using different concentrations of thermosensitive polymers (poloxamer407 alone or in combination with poloxamer 188) and methyl cellulose (MC ) or hydroxypropyl methylcellulose (HPMC K4M )in different concentrations used as mucoadhesive polymer and the resultant formulations were subjected to several tests such as gelation temperature GT, appearance and pH value. The formulas with the most appropriate GT were subjected to in-vitro drug release. Three formulas were chosen with appropriate release, F6 (15% P407, 1% MC), F29 (18%P407,3% P188, 0.8% HPMC) and F30 (18%P407,3% P188, 1% HPMC). These formulas were subjected to mucoadhesive force, viscosity, drug content, spreadability, gelation time and Fourier Transform Infrared (FTIR) compatibility studies. The results indicates that formula F29 and F30 have best gelation temperatures (33°C, 32°C) gel strength (1.5h,2h) mucoadhesive force of (17.1, 23.4 dyne/cm2 ) and in-vitro drug release (98.2%, 100%) respectively during 3.5h and gelation, time about 10 seconds for both formulas and FTIR spectrum study show absence of important interaction between secnidazole and the polymers used.

Development of Besifloxacin HCL Loaded Ocular İn Situ Gels; In Vitro Characterization Study

Objective: The aim of this study is to develop in situ gel formulations containing besifloxacin hydrochloride are heat triggered, which are prepared by using different poloxomer and derivatives different polymers that will change the gelling temperature to increase corneal contact time, regulate drug release, improve ocular bioavailability and increase patient compliance increase mucoadhesion.&#x0D; Material and Method: Various concentrations of poloxamer 188 (P188) and poloxamer 407 (P407) were used to create the in situ forming gels. To increase the gel's capacity for bioadhesion, mucoadhesives such hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were included in the formulations. Drug release in vitro, sol-gel transition temperature, rheological behavior, pH, clarity, and mucoadhesion force were all assessed for the produced formulations. &#x0D; Result and Discussion: The developed formulations' gelation temperatures ranged from 29 to 35°C. The preparations' viscosity and mucoadhesion force increased with increasing P407, HPMC, and HEC concentrations. Besifloxacin HCl forms in situ gel formulas with K1, K2, K3, and K6 suited for mucoadhesion characteristics, gelation temperature, and viscosity. These formulations exhibit pseudoplastic flow. Increasing polymer concentrations resulted in a reduction in the burst release of the formulations. However, at the end of 6 hours, drug release was finished in all formulations. The results show that in situ gels containing P407 and P188 show promise for besifloxacin HCl application