Invitro Drug Release Research Articles

Formulation Development of Mucoadhesive Vaginal Gel of Secnidazole and Voriconazole.

Purpose: Over the preceding decades, developing conventional drug delivery in to modified form has acquired importance in the pharmaceutical industry. Vaginal drug delivery system offers localized drug administration of drug and also avoids unwanted side effects of oral drug delivery. Vaginal drug delivery system has significant role in medical practice. Even though VDDS has a lot of advantages over the other routes of administration. The goal of developing the Mucoadhesive Vaginal Gel was to achieve the synergistic effect of voriconazole and secnidazole in the treatment of bacterial and fungal vaginal infections. Method: Mucoadhesive antimicrobial vaginal gel was optimised using Design expert software using Carbopol 934, HPMC K4M polymers. Result: Formulation was evaluated for various rheological parameters ,antimicrobial activity, invitro drug release and stability study. The spreadability and pH was found to be 5.5 to 7.4 cm and 4.12. Its compatible with vaginal pH. The selected optimized F8 formulation is the best formulation and the drug ratio is 2:1. and optimum gel viscosity is 1874 cps. antimicrobial study revealed that faster drug release of test formulation was compared to marketed product. It indicates as inhibition zone. Conclusion: The combination of drugs can serves as better option for treating vaginitis, compared to single drug formulation. Mucoadesion increases contact time of drug with affected area which rendered formulation more effective.

Responding to Hitch in Fighting Mycobacterium Tuberculosis Through Arginine Multi Functionalized Mucoadhesive SNEDDS of Rifampicin.

The study aimed to develop thiolated pluronic-based self-emulsifying drug delivery system (SNEDDS) targeted delivery of Rifampicin coated by arginine for enhanced drug loading, mucoadhesion, muco penetration, site-specific delivery, stabilized delivery against intracellular mycobacterium tuberculosis (M. tb), decreased bacterial burden and production by intracellular targeting. Oleic oil, PEG 200 and Tween 80 are selected as oil, co-surfactant and surfactant based on solubilizing capacity and pseudo ternary diagram region. Coating of thiolated polymer on SNEDDS with ligand arginine (Arg-Th-F407 SNEDDDS) decreased bacterial burden and production by intracellular targeting in macrophages. Formulation are evaluated through scanning electron microscope (SEM), EDAX analysis, diffraction laser scattering (DLS), Fourier transform infrared (FTIR) spectroscopy, and thermal analysis (DSC & TGA). Hydrodynamic diameter of thiolated polymeric SNEDDS (Th-F407 SNEDDS) and Arg-Th-F407 SNEDDS is observed to be 148.4 and 188.5nm with low PDI of 0.4 and 0.3, respectively. Invitro drug release study from Arg-Th-F407 SNEDDS indicates 80% sustained release in 72h under controlled conditions. Arg-Th-F407 SNEDDDS shows excellent capability of killing M.tb strains in macrophages even at low dose as compared to traditional rifampicin (RIF) and is found biocompatible, non-cytotoxic, and hemocompatible. Therefore, Arg-Th-F407 SNEDDDS of RIF proved ideal for targeting and treating M.tb strains within macrophages.

QBD approach for green synthesis of Rutin silver nanoparticles- screening for antioxidant, anticancer and anticlastogenic potential

Rutin is a flavonoid glycoside abundant in many plants exhibiting pharmacological activities like antioxidant, anticancer, anti-inflammatory and antimicrobial activities. Plant biomarkers suffer low bioavailability and solubility that lack clinical effectiveness. The smart nanoparticles conversion addresses this limitation with optimal particle size and targeted drug delivery. The present study involves QbD approach for formulation of Rutin silver nanoparticles and evaluation of antioxidant, anticancer and anticlastogenic potential. QbD experimentation involved particle size and drug release as dependent variables over the silver nitrate concentration, methanol and sonication time as independent variables devising 15 formulations (F1 –F15). F12 formulation was found to be optimized with 126.3 nm average size, stable and dispersible characterized by UV, FTIR, SEM and DLS studies. The calibration curve of Rutin was plotted at 352 nm with linearity (LOD = 0.061 μg/ml and LOQ = 0.187 μg/ml). The invitro drug release studies by USP dissolution apparatus I (Basket type) proved the sustained release characteristics with 97.3 % drug release when compared to the Rutin. The pharmacological screening for potential antioxidant and anticancer activity on G361 and MCF 7 cell line of F12 formulation have shown promising results and also enhanced solubility in water compared to Rutin. Anticalstogenic potential as a function of induced micronuclei frequency was evaluated as a characteristic feature in bone marrow cells obtained from mice. Results indicate pre-treatment with the F12 reduced frequency of micronuclei in mouse bone marrow cells caused by Cyclophosphamide (CP) significantly. The protective effect of F12 in suppression was demonstrated at both dosages of 100 and 200 mg/kg. Thus the findings suggest the novel Rutin silver nanoparticles as lead drug serving as antioxidant, anticancer and anticlastogenic agent.

Variables Affecting the Preparation and Characterization of Axitinib as Oral Niosmoes

Axitinib is anticancer drug act on different solid tumors by inhibtion protein kinase enzyme which is responsible for support the tumors with blood demand. Due to its low solubility, it has low bioavailability when given orally also it is affected by liver metabolism. Axitinib formulated as non-ionic vesicles (niosomes) for the first time to study the effect of different variables on the in vitro behaviour of vesicles in a hope to improve drug oral bioavailability. Niosomal dispersion formulas were formulated by diverse techniques via multiple kinds of surface-active agent (tween also span), cholesterol and dicetyl phosphate then evaluated for visual appearance, efficiency of drug entrapment (EE%), size of the vesicles, poly dispersity index, zetapotential, viscosity, invitro drug release and study the vesicles morphology by FE-SEM. Many variables effect on EE% were studied such as effect of surfactant amount and type, effect of surfactant combination, impact of various ratios of cholesterol, impact of DCP in various amount , effect of preparation method and effect of sonication time. The results showed that the EE% between (50.97%-98.24%), the particle size was found within the range (64.5 nm - 530.79 nm), zeta potential which was between ( -16.6 to -31 mV), polydispersity index (PDI) <1 and viscosity between (584 – 889.6) centipoise. The niosomal dispersion F1 which contained 1:1 weight ratio (span60: cholesterol) was found with high EE% (96.5±0.16%), smallest particle size (64.5±0.5 nm), highest drug release (100%) of drug released at the end of 4 hours and FE-SEM photograph showed that niosomes were spherical with no aggregation and had a smooth surface. The results showed that thin film hydration method with sonication for four minutes was the best method for preparation of axitinib niosomes, the type and amount of surfactants used, cholesterol ratio, stabilizer and the time of sonication had a substantial effect on EE%, the size of the vesicles as well as drug release; which were investigated so as to optimize the niosomal dispersion of anti-tumour drug reaching to an optimum formula that may improve drug bioavailability. Key words: Axitinib, Anticancer, Vesicles, Surfactants, Invitro behaviour, Entrapment efficiency.

Oral inhalation of dacomitinib nanocarriers as a therapeutic strategy for non-small cell lung cancer.

Background: Development of an inhalable nanoformulation of dacomitinib (DMB) encapsulated in poly-(lactic-co-glycolic acid) nanoparticles (NPs) to improve solubility, facilitate direct lung delivery and overcome the systemic adverse effects.Methods: DMB-loaded poly-(lactic-co-glycolic acid) NPs were prepared using solvent evaporation and characterized for particle size, polydispersity index and zeta-potential. The NPs were evaluated for invitro drug release, aerosolization performance and in vitro efficacy studies.Results: The NPs showed excellent particle characteristics and displayed a cumulative release of ∼40% in 5days. The NPs demonstrated a mass median aerodynamic diameter of ∼3 μm and fine particle fraction of ∼80%. Further, in vitro cell culture studies showed improved cytotoxic potential of DMB-loaded NPs compared with free drug.Conclusion: The study underscores the potential of DMB-loaded NPs as a viable approach for non-small cell lung cancer treatment.

Development and characterization of ferulic acid-loaded chitosan nanoparticle embedded- hydrogel for diabetic wound delivery

Diabetic wounds present a significant global health challenge exacerbated by chronic hyperglycemia-induced oxidative stress, impeding the natural healing process. Despite various treatment strategies, diabetic foot ulceration lacks standardized therapy. Ferulic acid (FA), known for its potent antidiabetic and antioxidant properties, holds promise for diabetic wound management. However, oral administration of FA faces limitations due to rapid oxidation, stability issues, and low bioavailability. The topical application of FA-loaded chitosan nanoparticles (FA-CSNPs) has emerged as a promising approach to overcome these challenges. Here, we report the development of a sustained-release formulation of FA-CSNPs within a hydrogel matrix composed of Chitosan and gelatin. The FA-CSNPs were synthesized using the ionic gelation method andoptimized through a Central Composite Design (CCD) approach. Characterization of the optimized nanoparticles revealed spherical morphology, a particle size of 56.9 ± 2.5 nm, and an impressive entrapment efficiency of 90.3 ± 2.4 %. Subsequently, an FA-CSNPs-loaded hydrogel was formulated, incorporating chitosan as a gelling agent, gelatin to enhance mechanical properties and cell permeation, and glutaraldehyde as a cross-linker. Comprehensive characterization of the hydrogel included pH, moisture loss, porosity, swelling index, rheology, water vapor transmission rate (WVTR), SEM, TEM, invitro drug release studies, antioxidant activity, antibacterial efficacy, cell cytotoxicity, cell migration studies on L929 fibroblast cell line, and stability studies. The stability study demonstrated negligible variations in particle size, zeta potential, and entrapment efficiency over 60 days, ensuring the stable nature of nanoparticles and hydrogel. This innovative delivery approach embedded within a hydrogel matrix holds significant promise for enhancing the therapeutic efficacy of FA-CSNPs-hydrogel in diabetic wound healing applications.

Formulation and Evaluation of Taste Masked Chewable Tablet containing Curcumin, Acetaminophen, and Ascorbic acid to treat sore throat

Objective: This study was intended to investigate the formulation and characterization of Mesalamine or 5-Aminosalicylic acid (5-ASA) pellets using novel excipient and formulated as matrix spheres to controlled the drug release extended period of time. Uniformly distributed throughout the gastrointestinal tract and Avoid dose dumping of drug. Methods: Mesalamine's active pharmaceutical component was characterised, and investigations were conducted prior to formulation to ensure a physical combination of the drug and excipients was achieved. Formulation of mesalamine as matrix pellets by using fluid bed processor and mesalamine loaded into seal coated sugar spheres and extended-release coating with Ethyl cellulose. Ethyl cellulose is pH independent polymer and retarder the drug release throughout the gastrointestinal tract and site-specific action in colon. Hypromellose also act as pore former and drug release based on diffusion mechanism. In drug layering, core pellets contain stearic acid and hydrogenated castor oil internally forming a matrix. Developed mesalamine pellets are characterized such as drug content, invitro drug release and appearances and particle size distribution. Results: Development of Mesalamine pellets based on five strategy From MEZ 1 to MEZ 5 are formulated and Characterization are performed. Based on the invitro drug release studies, we concluded that the formulation MEZ-IV was best formulation. Invitro drug release is consistence throughout 12hours.(1hrs-23%, 2nd hrs 41%, 4hrs-73, 6hrs-86, 8hrs-99% and 12hrs-10.

Formulation Development and Evaluation of Floating Beads of Propranolol Hydrochloride

Purpose: The purpose of present research work was to prepare sodium alginate and pectin antihypertensive floating beads of propranolol hydrochloride. Methods: Floating beads were prepared by using Ionotropic gelation technique using various natural and synthetic polymers in different proportion like sodium alginate, pectin, hydroxy propyl methyl cellulose k4m and calcium carbonate. Result: The floating beads were formulated and evaluated to physiochemical studies, Entrapment efficiency, swelling index, Invitro drug release, drug content, buoyancy studies (Floating time, floating lag time, total floating time) on the basis of evaluation of all floating beads were show good results. Conclusion: It Concluded that floating drug delivery system are float immediately upon contact with gastric fluid for increasing the bioavailability of drug and patient compliance.

Pioglitazone Nanoparticles Development, Characterization, Optimization, and a Zebrafish Model Evaluation of its Teratogenic Safety

Background: New nanoparticles (NPs) and biomaterials are utilized more frequently in biological research for vaccinations, diagnostic procedures, and drug administration. Nanomaterials are materials with d50 value from 1 to 100nm. They are also found in various consumer goods, the environment, and work. Thus, it has become crucial for the appropriate development of nanotechnology to assess the safety and potential therapeutic applications of these nanomaterials. The BCS Cass II medication pioglitazone hydrochloride, used to treat hypoglycaemia, has poor bioavailability after oral treatment because it dissolves poorly in gastrointestinal fluids. background: New nanoparticles and biomaterials are utilized more frequently in biological research for vaccinations, diagnostic procedures, and drug administration. They are also found in various consumer goods, the environment, and work. Thus, it has become crucial for the appropriate development of nanotechnology to assess the safety and potential therapeutic applications of these nanomaterials. The BCS Cass II medication pioglitazone hydrochloride, used to treat hypoglycaemia, has poor bioavailability after oral treatment because it dissolves poorly in gastrointestinal fluids. Objective: This study aimed to create adjusted pioglitazone nanoparticles to decrease dose-related side effects and prolong its release when used against type 2 diabetes. objective: This study aimed to create adjusted pioglitazone nanoparticles to decrease dose-related side effects and prolong its release when used against type 2 diabetes Methods: The emulsion solvent evaporation approach was used to create nanoparticles utilising HPMC K15M and Eudragit S100 as polymers, and Tween 80 as a surfactant. On framed nanoparticles, in-vitro evaluation approaches for drug-polymer compatibility, percentage yield, particle size, zeta potential, polydispersity index, surface morphology, encapsulation effectiveness, and in-vitro drug release study were used, followed by in-vivo acute toxicity experiment. Conclusion: From the obtained data, it can be said that a suitable optimized formulation of pioglitazone nanoparticles was prepared, which offered extended drug release of 95% in 10 hours.

Assessment of the cytotoxic effect of carboxymethyl chitosan-loaded amygdalin nanoparticles against human normal and cancer cell lines

In recent years, the development of antitumor drugs has been dedicated to natural products. Amygdalin is a natural herbal cyanoglycoside that has anticarcinogenic effect on many types of cancers once hydrogen cyanide (HCN) is released. The main objective of the present study is to synthesize and investigate the potential of carboxymethyl chitosan nanoparticles (CMC NPs) as drug delivery agents for amygdalin encapsulation and its delivery to cancer and normal cell lines. In this study, carboxymethyl chitosan nanoparticles encapsulated with amygdalin (CMC-Am NPs) were prepared and characterized through their particle size, surface charge, chemical structure and dielectric properties. Also, the invitro drug release of amygdalin from CMC NPs was studied. Additionally, the cytotoxcity of the amygdalin and CMC-loaded amygdalin NPs were evaluated through MTT assay. The results showed that the prepared CMC-loaded amygdalin NPs exhibited a small particle size of 129 nm, high zeta potential value of − 43 mV and confirmed the amygdalin stability and compatibility with CMC NPs. Furthermore, the CMC NPs demonstrated sustained release of amygdalin during 24 h. Moreover, compared to free amygdalin, amygdalin-loaded CMC NPs have significant anti-cancerous effect on human colon HCT-116 and breast MCF-7 cancer cell lines while being safe on normal cells BJ1. In conclusion, CMC NPs can be employed as an efficient drug delivery vehicle for controlled and sustained amygdalin release with enhanced cytotoxicity on malignant cells without harming normal cells.

Levofloxacin loaded chitosan and poly-lactic-co-glycolic acid nano-particles against resistant bacteria: Synthesis, characterization and antibacterial activity

BackgroundWith the global increase in antibacterial resistance, the challenge faced by developing countries is to utilize the available antibiotics, alone or in combination, against resistant bacterial strains. We aimed to encapsulate the levofloxacin (LVX) into polymeric nanoparticles using biodegradable polymers i.e. Chitosan and PLGA, estimating their physicochemical characteristics followed by functional assessment as nanocarriers of levofloxacin against the different resistant strains of bacteria isolated from biological samples collected from tertiary care hospital in Lahore, Pakistan. MethodsLVX-NPs were synthesized using ion gelation and double emulsion solvent-evaporation method employing chitosan (CS) and poly-lactic-co-glycolic acid (PLGA), characterized via FTIR, XRD, SEM, and invitro drug release studies, while antibacterial activity was assessed using Kirby-Bauer disc-diffusion method. ResultsData revealed that the levofloxacin-loaded chitosan nanoparticles showed entrapment efficiency of 57.14% ± 0.03 (CS-I), 77.30% ± 0.08(CS-II) and 87.47% ± 0.08 (CS-III). The drug content, particle size, and polydispersity index of CS-I were 52.22% ± 0.2, 559 nm ± 31 nm, and 0.030, respectively, whereas it was 66.86% ± 0.17, 595 nm ± 52.3 nm and 0.057, respectively for CS-II and 82.65% ± 0.36, 758 nm ± 24 nm and 0.1, respectively for CS-III. The PLGA-levofloxacin nanoparticles showed an entrapment efficiency of 42.80% ± 0.4 (PLGA I) and 23.80% ± 0.4 (PLGA II). The drug content, particle size and polydispersity index of PLGA-I were 86% ± 0.21, 92 nm ± 10 nm, and 0.058, respectively, whereas it was 52.41% ± 0.45, 313 nm ± 32 nm and 0.076, respectively for PLGA-II. The XRD patterns of both polymeric nanoparticles showed an amorphous nature. SEM analysis reflects the circular-shaped agglomerated nanoparticles with PLGA polymer and dense spherical nanoparticles with chitosan polymer. The in-vitro release profile of PLGA-I nanoparticles showed a sustained release of 82% in 120 h and it was 58.40% for CS-III. Both types of polymeric nanoparticles were found to be stable for up to 6 months without losing any major drug content. Among the selected formulations, CS-III and PLGA-I, CS-III had better antibacterial potency against gram+ve and gram-ve bacteria, except for K. pneumonia, yet, PLGA-I demonstrated efficacy against K. pneumonia as per CSLI guidelines. All formulations did not exhibit any signs of hemotoxicity, nonetheless, the CS-NPs tend to bind on the surface of RBCs. ConclusionThese data suggested that available antibiotics can effectively be utilized as nano-antibiotics against resistant bacterial strains, causing severe infections, for improved antibiotic sensitivity without compromising patient safety.

Formulation and Evaluation of Invasomal and Ethosomal Gel for Curcumin and Determination of Anti- Fungal Activity

Background: Despite exhibiting anti-inflammatory, antiseptic, and anti-cancer properties, curcumin is not exhibiting the same efficacy as that other non-steroidal anti-inflammatory agents and anti-cancer drugs. The main reason is its poor solubility and poor permeability. To improve the solubility the particle size has to be reduced to the nano level and to improve the permeability vesicular drug delivery approaches have to be adapted. By developing invasomal and ethosomal gels the bioavailability of curcumin can be enhanced. Aim and Objective: The main aim of the study is to develop Invasomal and Ethosomal drug delivery systems for curcumin by various techniques. Methods: Curcumin loaded invasomes were prepared by using a thin film hydration method. Six formulations were prepared by varying drug to lipid ratios (INV1 to INV6). Soya lecithin was used as a phospholipid, span60 was used as a surfactant, limonene was used as terpene, ethanol and chloroform were used as solvents. Curcumin-loaded ethosomes were prepared by using a hot method. Five formulations were prepared by increasing lipid concentration (E1 to E5). Soya lecithin as lipid, propylene glycol, and ethanol as solvent. The prepared formulations were evaluated for particle size, zeta potential, drug content, entrapment efficiency. and in vitro drug release studies. Results: Among all the formulations of Invasomes, INV3 formulation containing a 1:5 ratio of the drug (40 mg) to lipid (200 mg) was considered as best formulation because of its particle size of 327. A total of 1nm, zeta potential of -32.6 mV, highest drug content of 97.5%, entrapment efficiency of 96%, and in vitro drug release of 95% in a time period of 12 hrs. Among all the formulations of ethosomes, the E3 formulation was considered as best formulation due to its particle size of 697.5 nm, zeta potential of - 28.0 Mv, highest drug content of 97.3%, entrapment efficiency of 90%, and in vitro drug release of 94.6% in a time period of 12 hrs. Conclusion: The best invasomal and ethosomal formulations were incorporated into gel and evaluated for pH, viscosity, Spreadability, drug content, in vitro drug release studies, and ex vivo studies. INV3 and E3 were incorporated into gel and comparative studies were made with plain gel. Among the three gels (PG, INV3G, E3G), invasomal gel (INV3) exhibited the highest content drug content of 81%, pH of 6.6, spreadability 14.8g cm/sec, in vitro drug release of 90.6%, ,and ex vivo drug release of 97% in a time period of 12 hrs with the release rate of 32.53 microgram/cm2/hr-1/2, the flux of 0.346 μg/cm2/hr and permeation coefficient of 42.71 cm/hr.

Synthesis and invitro antitumor activity of galactosamine-docetaxel conjugates.

Docetaxel (DTX) is a semi-synthetic analogue of paclitaxel which has attracted extensive attention in the treatment of cancer. However, the current clinically used DTX formulations display low tumor targeting ability, leading to unsatisfactory therapeutic outcomes with adverse effects, which poses significant challenges to the clinical application. In this study, three galactosamine (Gal) and docetaxel conjugates with different linkers were synthesized, namely DTX-(suc-Gal)2, DTX-(DTDPA-Gal)2, and DTX-(DSeDPA-Gal)2. These three conjugates were characterized by 1H NMR, FT-IR and HRMS. The invitro drug release study shows that DTX-(DTDPA-Gal)2 and DTX-(DSeDPA-Gal)2 exhibit glutathione (GSH)-responsive drug release and DTX-(DSeDPA-Gal)2 displays higher GSH-responsiveness. The invitro antitumor activity study shows that DTX-(DTDPA-Gal)2 and DTX-(DSeDPA-Gal)2 exhibit enhanced cytotoxicity, cell apoptosis rate and G2/M phase arrest against HepG2 cells as compared to DTX-(suc-Gal)2, DTX-(DSeDPA-Gal)2 displays the highest cytotoxicity, cell apoptosis rate and G2/M phase arrest among these three conjugates. In addition, DTX-(DSeDPA-Gal)2 exhibits higher selectivity to HepG2 cells as compared to free DTX. The DTX-(DSeDPA-Gal)2 developed in this study has been proven to be an effective DTX conjugate for selective killing hepatoma cells.

Design, Evaluation and Optimization of Albuterol Sulphate and Theophylline Pulsincap drug delivery system for chronotherapy of Asthma

The aim of the current study was to design and develop and evaluate pulsatile drug delivery system of Albuterol Sulphate and Theophylline for the treatment of Asthma. The capsule body was made water insoluble by cross linked with formaldehyde vaopur. The treatment of Formalin was adopted to modify the gelatin capsule solubility. The formalin residue was carried out by quantitative test. The drug-excipient compatibility is done by FTIR and UV . The pulsincap formulation were prepared by using hydrogel plug of various components. The drug content of the formulation of pulsincap was found to be in the general range. The invitro drug release studies in ph1.2 .6.2 and 7.4 buffern was noticed to be zero percent and capsule was stable for 2 hours drug the studyF5 formulation batch was selected which was best and good formulation and promoted maximum drug release of 96.29% percentage at phosphate buffers when compared with other formulation. Pulsincap formulation can be adopted for optimum delivery of pellets in the treatment as per chronotherapy
 Keywords: Theophylline, quantitative test, invitro drug release studies, phosphate buffers6.2 and 7.4.

Design, Formulation, and Evaluation of Lisinopril Mucoadhesive Buccal Patches by Using the Combination of Natural Polymers

The main objective of present investigation to formulate and evaluate mucoadhesive buccal patches of Lisinopril using solvent casting method. Sodiumalginate combined with Sodium carboxyl methyl cellulose, HPMC, and Carbopol934 in different proportions were used as a mucoadhesive polymer and Propyleneglycol used as a plasticizer as well as penetration enhancers. The formulated Buccal patches of Lisinopril were evaluated on the basis of Thickness, Weight uniformity, folding endurance, swelling Studies, Surface pH Determination, Percentage Moisture loss, Drug content Uniformity, Ex-Vivo Mucoadhesive strength, In Vitro Drug Release, Ex- vivo permeation study. By compatibility study there is no chemical interaction between drug and excipients used. All prepared buccal patches were transparent, smooth, consistent and flexible. The surface pH of all formulations was found to be almost in neutral pH and no mucosal irritation was expected. Among all the formulations, F6 showed maximum swelling index as 25.01%. The optimized formulation F6 also showed satisfactory, Mucoadhesive strength (5.1kg/cm2), drug content (98.75), and Ex-Vivo permeation (82.03%). In-Vitro drug release of optimised formulation (F6) was found to be 75.12 at the end of 8 hrs. Drug release mechanism was determined by plotting release data to Higuchi and Korsmeyer-Peppas model. All the formulations are best fitted to Korsmeyer-Peppas model and according to this model the drug releases from theses patches may be controlled by diffusion with super case-II transport.

Formulation and evaluation of Glibenclamide loaded Nanosponges

Nanotechnology mediated drug delivery has been reported to enhance the drug efficacy, bioavailability, reduced toxicity and improve patient compliance by targeting the cells and tissues to elicit the desired pharmacological action. The main aim of the study was to formulate Glibenclamide loaded nanosponges and to evaluate them. Glibenclamide loaded nanosponges were prepared by Emulsion solvent diffusion method using different polymers (Ethyl cellulose, β- cyclodextrin, Hydroxy Propyl β- cyclodextrin, Pluronic F68). The FTIR test is conducted as the preliminary test, by this test there was no interaction between the drug and polymers. Then nanosponges were evaluated for particle size, PDI, zeta potential, SEM, entrapment efficiency and invitro drug release. The particle size ranged from 640.7 to 876.2 nm, PDI ranged from 0.456 to 0.707, zeta potential from -17.3 to -34.3 mV and entrapment efficiency was ranged from76.21 to 98.23% The cumulative percentage release from all nanosponges varied from 80.35 to 97.56% after 12 hours depending upon the drug and polymers ratio and F5 formulation showed highest drug release i.e., 97.53%. The release kinetic studies showed that the release first order diffusion controlled and the n value (0.8769) from the Korsmeyer- Peppa’s model indicated the release mechanism was non-fickian type.

Fabrication of dual drug-loaded polycaprolactone-gelatin composite nanofibers for full thickness diabetic wound healing.

Aim: Design of moxifloxacin and ornidazole co-loaded polycaprolactone and gelatin nanofiber dressing for diabetic wounds. Materials & methods: The composite nanofibers were prepared using electrospinning technique and characterized for in vitro drug release, antibacterial activity, laser doppler and in vivo wound healing. Results: The optimized nanofiber demonstrated an interconnected bead free nanofiber with average diameter <200nm. The invitro drug release & antimicrobial studies revealed that optimized nanofiber provided drug release for >120h, thereby inhibiting growth of Escherichiacoli and Stapyhlococcusaureus. An in vivo wound closure study on diabetic rats found that optimized nanofiber group had a significantly higher wound closure rate than marketed formulation. Conclusion: The nanofiber provided prolonged drug release and accelerated wound healing, making it a promising candidate for diabetic wound care.

Formulation and Evaluation of Herbal Transdermal patches for Rheumatoid arthritis

The allopathic healthcare system provides two conventional ways of treatment for rheumatoid arthritis, both of which have side effects. As a result, turning to Ayurvedic herbal treatment formulation that is safe, effective, and proven would be a better choice. Rheumatoid arthritis is an autoimmune disease that is chronic and progressive ,distinguished by chronic inflammation affecting the peripheral joints. Transdermal films containing herbal medicinal plants such as Cardiospermum helicacabum and Aloe barbadensis were designed in this study to treat rheumatoid arthritis . The solvent casting method was used to develop transdermal patches using plant extracts. The patches were evaluated based on physicochemical parameters such as thickness, folding endurance, physical appearance, weight uniformity, moisture content, drug content, flatness, moisture uptake, pH, and invitro drug release and stability study. The plots for average absorbance release vs time through transdermal film shows that drug release occurred at a steady rate. The skin irritation study on human volunteer's skin revealed that the formulation does not cause skin irritation. Overall, the present research provides a novel approach to the implementation of transdermal drug delivery techniques in the design of herbal remedies.

Innovative Nanosuspension Formulation for Prochlorperazine and In-vitro Evaluation

Prochlorperazine is a dopamine antagonist and is used to control nausea and vomiting. It is a BCS class II drug which has low aqueous solubility and high permeability. The present study is aimed to formulate and evaluate prochlorperazine nanosuspension to improve solubility and enhance dissolution of Prochlorperazine with varying concentrations of stabilizers such as Tween 80, PVP K30, Poloxamer 188 by using nanoprecipitation method. The developed formulations were characterized for particle size and polydispersity index, total drug content, SEM, Zeta Potential and FTIR. The invitro drug release studies and invitro drug release kinetics were performed for all formulations. FTIR studies revealed that drug is compatible with the excipients. The particle size and poly dispersity index of optimized formulation was found to be 162nm and the zeta potential was found to be -30.2 mV and concluded that the system had sufficient stability. The invitro drug release was found within their acceptable ranges. The rate of dissolution of best batch was enhanced to 93.24 in 120min. Stability studies proved that nanosuspensions were more stable with no significant changes in particle size distribution. Thus the formulated nanosuspension of prochlorperazine offers a superior conventional dosage forms for drug release&#x0D; Keywords: Prochlorperazine, Nanosuspension, Solubility, Dissolution

Formulation of Methotrexate Loaded Solid Lipid Nanoparticles By Micro Emulsion Technique

AIM: The aim of this study was to develop and characterize Methotrexate loaded solid lipid nanoparticles by Microemulsion technique. Background: Methotrexate is a preferable anti metabolite drug. It is used in the treatment of certain cancers like breast cancer, skin and lung cancer. Clinical studies have revealed that the curative effect of MTX tablet on cancers was limited due to their toxic dose-related side effects to normal cells, nephrotoxicity, and bone marrow suppression, acute and chronic hepatotoxicity and also due to the drug resistance of the tumour cells. Hence, there is a need to develop methotrexate solid lipid nanoparticles in order to minimize the adverse effects associated with the MTX tablet dosage form. Objective: The objective of the research work is to formulate, characterize and evaluate Methotrexate solid lipid nanoparticles by micro emulsification solidification technique. Methods: Solid lipid nanoparticles are prepared by using lipids stearic acid and glycerol monostearate by varying the concentration of surfactant. Three formulations were prepared with each lipid. Micro emulsion technique was adopted for the preparation of solid lipid nanoparticles. Each formulation was evaluated for drug content, entrapment efficiency, loading capacity&amp; invitro drug release studies. Both the lipids were compared for the characterization and evaluation parameters. Result: On comparison Glycerol monostearate was found to be a better lipid over Stearic acid for the preparation of Methotrexate solid lipid nanoparticles because of its smaller mean particle diameter (238.8 nm), higher stability (-56.5 mV) and greater entrapment efficiency. Conclusion: Methotrexate solid lipid nanoparticles were successfully prepared with higher stability and drug release rate.