scholarly journals FORMULATION AND EVALUATION OF GEL LOADED WITH MICROSPHERES OF APREMILAST FOR TRANSDERMAL DELIVERY SYSTEM

2019 ◽  
pp. 411-417
Author(s):  
N. V. SAI PRIYANKA ◽  
P. NEERAJA ◽  
T. MANGILAL ◽  
M. RAVI KUMAR
Keyword(s):  
Research Work ◽  
Gel Strength ◽  
Gelling Agent ◽  
Stability Studies ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Diffusion Studies ◽  
In Vitro Diffusion ◽  
Drug Kinetics

Objective: The main objective of the present research work was to formulate and evaluate gel loaded with microspheres of apremilast to increase bioavailability and to reduce the dosing frequency and to improve patient compliance. Methods: Gel loaded with microspheres of apremilast was prepared by solvent evaporation method by taking different ratios of polymers. Ethyl cellulose as a polymer, dichloromethane solvent is used as drug solubility, polyvinyl alcohol as a surfactant, and sodium alginate is used as gelling agent. Prepared gel loaded with microspheres was evaluated for drug interactions by Fourier transform infrared (FTIR), differential scanning calorimetry studies, and surface morphology by scanning electron microscopy (SEM), to select effective one among all formulations. The prepared formulations (F1–F6) were evaluated for pre-formulation studies, spreadability, viscosity, pH measurement, gel strength, homogeneity, drug content, in vitro diffusion studies, drug kinetics, and finally for stability studies. Results: Differential scanning calorimeter studies confirmed that there is no drug interaction between drug and excipients. FTIR spectroscopy studies confirmed that there is compatibility between drug and excipients. Regular and spherical shape particles with smooth surface were observed in the SEM photographs. The optimized gel loaded with microspheres of F4 formulation (drug: polymer in 1:4 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as spreadability (5.86±0.54 g.cm/s), viscosity (568 cps), pH (6.33±0.55), gel strength (38 s) and drug content (90.00±0.71%). In vitro diffusion studies have shown 80.1±1.92% drug release in 10 h. Drug kinetics follows zero order kinetics and n value was found to be 0.721. Stability studies were done for 3 months. Conclusion: All the results show that the gel loaded with microspheres of apremilast can be effectively used for the treatment of psoriasis and psoriatic arthritis.

scholarly journals Evaluation of antipsoriatic activity of gel containing Pongamia pinnata extract on Imiquimod-induced psoriasis

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Kamlesh Wadher ◽  
Shital Dabre ◽  
Anjali Gaidhane ◽  
Sagar Trivedi ◽  
Milind Umekar
Keyword(s):  
Mouse Model ◽  
Pongamia Pinnata ◽  
Gelling Agent ◽  
Proper Treatment ◽  
Phytochemical Screening ◽  
Diffusion Studies ◽  
In Vitro Diffusion ◽  
Gel Formulations ◽  
Disease And Disorders

Abstract Background Pongamia pinnata (Fabaceae) is among those categories of plants mentioned in Ayurveda and traditionally known to use in several types of disease and disorders. The objective of the present work was to investigate the anti-psoriatic activity of Pongamia pinnata leaves extracts in Herbal gel formulation. Results Hydroalcoholic leaves extract of Pongamia pinnata was first subjected to phytochemical screening and quantification of phytoconstituents. Herbal gel was prepared containing Pongamia pinnata extracts using Carbopol 934 as gelling agent. The prepared gel formulations were studied for pH, viscosity, Spreadability and in vitro diffusion studies. The imiquimod-induced psoriatic mouse model, showed a prominent anti-psoriatic activity of the extract as evident through index grading. Treatment with extract confirmed a noteworthy reduction in psoriasis in the treated groups as there was a considerable diminution in the thickness and scaling of skin. Conclusions Lack of proper treatment and disadvantages associated with allopathic medicines pave the way to extensive research in natural products with anti-psoriatic activity. The present research scientifically justified the anti-psoriatic activity of the Hydroalcoholic extracts of Pongamia pinnata leaves.

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

scholarly journals Fabrication and In Vitro Evaluation of pH-Sensitive Polymeric Hydrogels as Controlled Release Carriers

Gels ◽  
2021 ◽  
Vol 7 (3) ◽  
pp. 110
Author(s):  
Muhammad Suhail ◽  
Chih-Wun Fang ◽  
Arshad Khan ◽  
Muhammad Usman Minhas ◽  
Pao-Chu Wu
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Acrylic Acid ◽  
Chondroitin Sulfate ◽  
Diclofenac Sodium ◽  
Research Work ◽  
Controlled Delivery ◽  
Scanning Calorimetry ◽  
Release Studies

The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

scholarly journals Formulation and evaluation of in-situ gels enriched with Tropicamide loaded solid lipid nanoparticles

2018 ◽  
Vol 9 (1) ◽  
pp. 216
Author(s):  
Jayachandra Reddy Peddappi Reddigari ◽  
Yerikala Ramesh ◽  
Chandrasekhar B. Kothapalli
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Research Work ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Adhesive Force ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Diffusion Studies

The present research work “Formulation and Evaluation of In-situ gels enriched with Tropicamide loaded solid lipid nanoparticles”. To overcome the problems of side effects and to increase the bioavailability of tropicamide loaded solid lipid nanoparticles are containing with suitable lipids (glycerin trimyristate, Tristearin, Phosphatidylcholine & soyabean lecithin) with stabilizers (poloxamer 188) and surfactant like polysorbate 80. The interaction between drug, lipids & polymer by performing with FTIR no incompatibility with each other. The particle morphology was carried out by SEM & AFM in solid lipid nanoparticle formulation. The particle size was ranges from 213.6 ± 2.16nm to 538.0 ± 6.53 nm. The zeta potential ranges form -18.3mV to 25.6mV. The entrapment efficiency of free tropicamide was ranges from 74.13 % to 90.17%. The drug content was ranges from 0.212mg/ml to 0.912mg/ml. The SLN formulations must be transparent white colour and semi solid consistency. The pH 7.0 to 8.0 in all formulation. The gelling strength of gels TSLNGF1 to TSLNGF12 was ranges from 72 ± 1 sec to 117 ± 2 sec. The bio adhesive force was ranges from 10.12 ±1.01 dynes/cm2 to 23.12 ± 1.91 dynes/cm2. The viscosity of prepared formulation ranges from 415 ± 1.94 cps to 652 ± 1.41 cps. The spread ability studies of all formulation were ranges from 09 gms/sec to 18 gms/sec. The Accelerated stability the formulations does not undergo any chemical Changes. In vitro Franz’s diffusion studies of SLN enriched in gels TSLNGF1 to TSLNGF12 among the various formulation best formulations was TSLNGF6; its follows first order kinetics. Keywords: Solid Lipid Nanoparticles; Tropicamide; In- situ gels; In vitro diffusion studies

scholarly journals Development, Optimisation and Evaluation of Ketoprofen Lipospheres

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1853-1863
Author(s):  
Shubhra Rai ◽  
Gopal Rai ◽  
Ashish Budhrani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Research Work ◽  
Extended Period ◽  
Entrapment Efficiency ◽  
Inflammatory Activity ◽  
Scanning Calorimetry ◽  
Anti Inflammatory

Lipospheres represent a novel type of fat-based encapsulation system produced for the topical drug delivery of bioactive compounds. The goal of this research work was to develop lipospheres, including ketoprofen applied for topical skin drug delivery. Ketoprofen lipospheres were formulated by melt emulsification method using stearic acid and Phospholipon® 90G. The lipospheres were analysed in terms of particle size and morphology, entrapment efficiency, Differential scanning calorimetry, In-vitro drug release, In-vivo (Anti-inflammatory activity). Outcomes of research revealed that particle size was found to be 9.66 µm and entrapment efficiency 86.21 ± 5.79 %. In-vivo, the study of ketoprofen loaded lipospheres formulation shows a higher plain formulation concentration in plasma (5.61 mg/mL). For dermis, ketoprofen retention was 27.02 ± 5.4 mg/mL for the lipospheres formulation, in contrast to that of the plain formulation group (10.05 ± 2.8 mg/mL). The anti-inflammatory effect of liposphere drug delivery systems was assessed by the xylene induced ear oedema technique and compared with marketed products. Finally, it seems that the liposphere drug delivery system possesses superior anti-inflammatory activity as compared to the marketed product gel consistencies. Liposphere may be capable of entrapping the medicament at very high levels and controlling its release over an extended period. Liposphere furnishes a proper size for topical delivery as well as is based on non-irritating and non-toxic lipids; it’s a better option for application on damaged or inflamed skin.

scholarly journals FORMULATION AND EVALUATION OF ACYCLOVIR LOADED NOVEL NANO-EMULSION GEL FOR TOPICAL TREATMENT OF HERPES SIMPLEX VIRAL INFECTIONS

2018 ◽  
Vol 8 (5-s) ◽  
pp. 265-270
Author(s):  
Swati Patel ◽  
Prabhat Jain ◽  
Geeta Parkhe
Keyword(s):  
Herpes Simplex ◽  
Zeta Potential ◽  
Viral Infections ◽  
In Vitro Release ◽  
Stability Study ◽  
Oral Drug ◽  
Drug Content ◽  
Nanoemulsion Gel ◽  
In Vitro Diffusion

Acyclovir has low bioavailability mainly due to low solubility. This study aimed to formulate an optimized acyclovir (ACV) nanoemulsion gel for the slow, variable and incomplete oral drug absorption in patient suffering from herpes simplex viral infection. The dispersion solubility of acyclovir was studied in various oils, surfactants and co-surfactants and by constructing pseudo phase ternary diagram nanoemulsion area was identified. The optimized formulations of nanoemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in nanoemulsion, Zeta Potential and Vesicle size measurement and than nanoemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Span 40 was selected as surfactant, PEG 400 as co surfactant and castor oil as oil component based on solubility study. The in vitro drug release from acyclovir nanoemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of nanoemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of acyclovir can be increased by formulating into nanoemulsion gel. Keywords: Acyclovir, Nanoemulsion, In-vitro diffusion, Zeta potential, Stability

EFFECT OF DRUG TO B-CYCLODEXTRIN RATIO AND METHOD OF COMPLEXATION IN THE DEVELOPMENT OF B-CYCLODEXTRIN INCLUSION COMPLEX OF OFLOXACIN

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 34-40
Author(s):  
M Panchpuri ◽  
◽  
D Singh ◽  
A Semalty ◽  
M. Semalty
Keyword(s):  
Inclusion Complex ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Kneading Method ◽  
Made In

Ofloxacin, a second generation fluoroquinolone, shows poor aqueous solubility and dissolution profile. Thus, ofloxacin–β-cyclodextrin complexes were prepared to improve its dissolution by imparting an environment of improved hydrophilicity. Ofloxacin was complexed with β-cyclodextrin (in 1:1 and 1:2 molar ratio) by two different methods namely, solvent evaporation and kneading method. These inclusion complexes were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. The highest drug content (35.45%) was found in complex made by kneading method (OK1:1) in 1:1 molar ratio. All the complexes OSE1:1, OSE1:2, OK1:1, OK1:2 were found to be showing rough and porous surface morphology in SEM. Solubility as well as the dissolution of the complexes was found to be improved. Complex prepared by kneading method in 1:1 molar ratio (OK1:1) showed a marked improvement in percent drug release (88.94%) than that of pure drug (54.22%) at the end of 1 hour in dissolution study. FTIR, DSC and XRPD data confirmed the formation of inclusion complex. It was concluded that the complex made in 1:1 molar ratio (irrespective of the method) showed better solubility and dissolution profile as compared to complex made in 1:2 molar ratio.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

scholarly journals DESIGN, FORMULATION, AND CHARACTERIZATION OF APREMILAST-SACCHARIN COCRYSTALS LOADED WITH TOPICAL GEL

2020 ◽  
pp. 60-67
Author(s):  
TEJASWINI MANE ◽  
MUKESH MOHITE
Keyword(s):  
Physicochemical Properties ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Gelling Agent ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Topical Gel ◽  
Solubility Study

Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.

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