scholarly journals Formulation development and evaluation of antiacne activity of ethosomal gel prepared using Plumbago zeylanica root extract

2020 ◽  
Vol 11 (4) ◽  
pp. 5511-5516
Author(s):  
Sandhya P ◽  
Snehalata J
Keyword(s):  
Physicochemical Properties ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Root Extract ◽  
Formulation Development ◽  
Plumbago Zeylanica ◽  
Hydroalcoholic Extract ◽  
Drug Content ◽  
And Diffusion ◽  
Gel Formulations

The objective of present research work is, to develop an ethosome, as a carrier system for Plumbago root extract, its incorporation into gel formulations and to characterize the developed gel formulations by estimation of plumbagin content and study of antiacne activity. Roots of Plumbago zeylanica L (Plumbaginaceae) contains Plumbagin and is used for skin infections and intestinal worms. Topical therapy for acne includes comedolytic agents, antibiotics and anti-inflammatory drugs. The excessive use of antibiotics has led to the increased resistance of acne-causing bacteria. In this research work, plumbago roots have been screened for their potential use for the treatment of acne and hydroalcoholic extract of the roots was found to be effective. Seven batches (EF1-EF7) of ethosomes were prepared using soya lecithin (1-3%) and ethanol (10-45%) and the hydroalcoholic extract. The range of entrapment efficiency varied from 17.12 to 80.82%. The ethosomes EF6 having highest entrapment efficiency was incorporated into gel formulation. Carbopol 934P (0.5 -2%) was used to prepare ethosomal gel and evaluated for physicochemical properties, drug content and diffusion characteristics. The pH of the gel was in the range of 6.87 to 7.03. Viscosity was between 5600 - 9800 centipoises. The % drug content was in the range of 95.91% to 100.7%. The ethosome, in their gel formulation, showed good physicochemical properties, drug content and diffusion pattern. The anti-acne activity of F3 showed good zones of inhibition comparable with standard Clindamycin. The present study suggested ethosomal gel as an efficient carrier for plumbago root extract for antiacne activity.

Design and Development of Lomustine Loaded Chitosan Nanoparticles for Efficient Brain Targeting

2020 ◽  
Vol 18 (1) ◽  
pp. 45-54 ◽  
Author(s):  
Anupriya Anand ◽  
Bharadhwaj Ramesh Iyer ◽  
Chandrasekar Ponnusamy ◽  
Rajesh Pandiyan ◽  
Abimanyu Sugumaran
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
P Value ◽  
Drug Content ◽  
Diffusion Controlled

Aim: The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design. Methods: The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release. Results: The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1. Conclusion: In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.

Liquisolid Orodispersible Tablets of Valeriana officinalis L. Root Extraction: Formulation, Development, and Evaluation

2021 ◽  
Vol 16 ◽  
Author(s):  
Hossein Asgarirad ◽  
Ali Farmoudeh ◽  
Shervin AmirKhanloo ◽  
Amirhossein Babaei ◽  
Seyyedeh Saba Hosseini ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Chemical Interaction ◽  
Culture Media ◽  
Tween 80 ◽  
Water Soluble ◽  
Root Extract ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Orodispersible Tablets ◽  
Valerenic Acid

Background: Valerian root extract is used in traditional medicine to treat sleep disorders. According to previous studies, sedative effects are related to the presence of valerenic acid. Formulating orodispersible tablets (ODTs) is an effective and cost-benefit technique for accelerating drugs' therapeutic effects. This study aimed to formulate ODTs of valerian root extract and evaluate their properties. Materials and Methods: Valerian root was extracted by percolation in 70% ethanol. The solubility of valerenic acid was investigated in various liquid carriers. The extract was uniformly dispersed in the selected carrier (Tween 80), then mixed with other excipients and compressed into tablets. Fourteen formulations with different amounts of sodium starch glycolate (SSG, as a super disintegrant) and camphor (as a sublimating agent) were prepared. The physicochemical properties of the ODTs, drug release rates, and microbial limit tests (MLTs) were studied. Results: Both SSG and camphor accelerated tablet disintegration rates, and their composition showed a synergistic effect (P<0.05). The infrared spectroscopy revealed no chemical interaction between formulation components. The MLTs confirmed that a limited number of microbial colonies were grown in the liquid medium, and no pathogen growth occurred in the specific culture media. Conclusion: The results revealed that Valerian ODT's physicochemical properties were significantly improved compared to conventional tablets. The technique can be utilized for other poorly water-soluble pharmaceuticals.

scholarly journals FORMULATION AND EVALUATION OF LIPOSOMAL GEL CONTAINING EXTRACT OF PIPRINE

2020 ◽  
pp. 126-129
Author(s):  
YOGESH S. THORAT ◽  
NAGESH S. KOTE ◽  
VIRENDRA V. PATIL ◽  
AVINASH H. HOSMANI
Keyword(s):  
Room Temperature ◽  
Research Work ◽  
Herbal Extract ◽  
Piper Nigrum ◽  
Lipid Film ◽  
Hydroalcoholic Extract ◽  
Skin Repair ◽  
Pharmacological Potential ◽  
Herbal Formulations ◽  
Gel Formulations

Objective: The objective of present research work is to develop Liposomes as a carrier system for 70% Hydroalcoholic extract, its incorporation in to gel formulations and to characterize the prepared and develop Liposomal gel formulation. There are many reports revealing the pharmacological potential of Piper Nigrum. Methods: Cholestrol in various weight ratios were dissolved in 10 ml of Methanol: Chloroform (1:1) ratio used as a solvent. The extract solution was taken in a 500 ml round bottom flask. The flask was rotated in rotary flash evaporator at 40 rpm for 20 min in the thermostatically controlled water bath at 40 °C under vacuum 240 mmHg. The solvent was slowly removed by this process, and a very thin film of dry lipids was formed on the flask. The dry lipid film was slowly hydrated with 10 ml of Saline Phosphate Buffer pH 7.4 containing Insulin Drug. The flask was once again rotated at the same speed as before and at room temperature for 2 hr. The liposomal was left to overnight at 4°C, full lipid hydration. Results: This study was done for herbal formulations used for topical delivery of therapeutic agents at the time of injury to accelerate skin repair in the shortest time possible, with minimal pain. Plant Piper Nigrum. Family Piperaceac is extensively used. Conclusion: The present study revealed liposomal gel as an efficient carrier for herbal extract. Keywords: Piperine, Gel, Herbal extract, Liposomes, Liposomal gel.

scholarly journals Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization

2021 ◽  
Vol 3 ◽  
Author(s):  
Yang Xin ◽  
Shi Yun ◽  
Lu Yuhe ◽  
Mao Yinxue ◽  
Niu Shurui ◽  
...  
Keyword(s):  
Droplet Size ◽  
High Performance ◽  
Ternary Phase Diagram ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Isopropyl Myristate ◽  
Formulation Development ◽  
Drug Content ◽  
Light Yellow ◽  
Light Yellow Color

In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testing, and pseudo ternary phase diagram generation were implemented for screening components and optimized adopting the central composite design. While the tested responses were solubility, droplet size and PDI, thirteen trials were performed using two different variables, oil percentage and optimized emulsifier and co-emulsifier ratio. Microemulsions were then characterized for droplet size, PDI, transmission electron microscopy, viscosity, electrical conductivity, pH, entrapment efficiency, drug content and stability. Additionally, skin release profile, percutaneous absorption and retention were investigated adopting Franz diffusion cell. The optimal formulation was found to compose of laureth-9 (emulsifier, 6.72 g), propylene glycol (co-emulsifier, 1.80 g), isopropyl myristate (IPM, oil, 1.48 g), LFs (1.50 g) and at least more than 85% deionized water. The optimized and storage for 3 months of microemulsion was found to clear, light yellow color without phase separation or precipitation indicated the stability of the preparation to long-term placement. The mean droplet size, PDI, entrapment efficiency and drug content were discovered as 12.68 ± 0.12 nm, 0.049 ± 0.005, 97.28 ± 0.13% and 122.67 ± 0.40 mg·g−1, respectively. Furthermore, the optimal formulation sustained release LFs, remarkably deliver more LFs through the skin layer (644.95 ± 6.73 μg cm−2) and significantly retained LFs in the skin layer (9.98 μg cm−2). The study concluded that optimized microemulsion has potential and enhanced the dissolvability and cumulative penetration amount of LFs.

scholarly journals Application of Design of Expert software for evaluating the influence of formulation variables on the encapsulation efficacy, drug content and particle size of PEO-PPO-PEO/Poly(DL-lactide-co-caprolactone) nanoparticles as carriers for SN-38

2021 ◽  
Author(s):  
Rozafa Koliqi ◽  
Pranvera Breznica ◽  
Arlinda Daka ◽  
Blerina Koshi
Keyword(s):  
Ethylene Oxide ◽  
Water Solubility ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Formulation Development ◽  
Drug Content ◽  
Poly Ethylene Oxide ◽  
Drug Entrapment Efficiency ◽  
Poly Ethylene ◽  
Poly Propylene

Background and aims. Hydrophobic substances are mainly encapsulated into polymer nanocarriers in order to improve their solubility, enable their administration, at the same time to empower targeted tissue or cell specific delivery of the drug using the encapsulating vehicle as targeting and controlled release platform. 7-Ethyl-10-hydroxycamptothecin (SN-38) is an active metabolite of Irinotecan, showing 100- fold to 1000-fold higher effect than Irinotecan, but its clinical use is limited because of its extreme hydrophobicity, as it is practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. Method. In order to fully exploit the potential of the nanoprecipitation as a method for preparation of Poly(DL-lactide-co-caprolactone)- poly(ethylene oxide) - poly(propylene oxide) - poly(ethylene oxide) (P(DL)LCL/PEO-PPO-PEO) nanoparticles and evaluate the influence of the polymer P(DL)LCL, stabilizing agent PEO-PPO-PEO copolymer (Lutrol F127) and the drug concentration (SN-38) upon drug entrapment efficiency, size and drug content, a D-optimal experimental design for response surface using Design Expert Version 9.0.4.1. software investigation was created and statistically analyzed. Results. We have observed that at higher SN-38 concentration during the preparation procedure (nanoprecipitation, solvent diffusion method), and due to its extremely low water solubility, the drug will start to precipitate as unprotected crystals at a faster pace compared to polymer aggregation, leading to extremely low encapsulation efficacy and waste of the active compound. The most desirable combination of factor settings are SN-38=0.5 mg, Polymer=5mg and F127=4%. Conclusion. This investigation utilizes the design of experiment approach and extends the primary understanding of impact of formulation development of P(DL)LCL/PEO-PPO-PEO nanoparticles as carriers for SN-38.

scholarly journals Preparation, Characterization and In-Vitro Diffusion Study of Different Topical Flurbiprofen Semisolids

2020 ◽  
Vol 10 (01) ◽  
pp. 81-87
Author(s):  
Saba A. Jaber ◽  
Halah T. Sulaiman ◽  
Nawal A. Rajab
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Diffusion Study ◽  
In Vitro Drug Release ◽  
Gelling Agents ◽  
Drug Content ◽  
And Diffusion ◽  
Gel Formulations

Flurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best one. Method: Topical semisolid FLB preparations were formulated using different semisolid formulation starting from emulsion bases w/o and o/w comparing with different gelling agents in different concentrations which include carbopol 934, sodium carboxy methylcellulose (SCMC) and combination of both polymer in different concentration to get 1% gelling agents. All the gel formulations were evaluated for physical appearance, pH, spreadability, rheological studies, drug content, in vitro release and diffusion studies. Results: All gel formulations which contain gelling agent exhibit better in vitro drug release and permeation compared with the emulsion bases, especially 1% polymer combination. Ethanol exerts a significant effect (p less than 0.05) on the in vitro drug release and diffusion for 2% carpbopol 934 compared with SCMC. Drug content was found to be uniform in all the formulations. The pH ranges of formulated gels were found to be suitable for topical application. Conclusion: Based on overall results, FLB can be successfully prepared as topical semisolid preparation with accepted properties.

scholarly journals Formulation and Evaluation of Brimonidine Maleate Nanolipid in Situ Gel

2020 ◽  
Vol 11 (4) ◽  
pp. 7071-7077
Author(s):  
Mohd Azharuddin ◽  
Theivendren Panner Selvam ◽  
Maya Sharma ◽  
Jayesh Dwivedi
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Entrapment Efficiency ◽  
In Situ Gel ◽  
Visual Appearance ◽  
Carbopol 940 ◽  
Ocular Bioavailability ◽  
Release Data ◽  
Gel Formulations

The main objective of present research work was aimed to formulate and evaluate the nano lipid-based drug delivery system by incorporating a brimonidine maleate drug for ocular therapy. The patient can be improved by preparing nano lipid in situ gel as a vehicle by reducing the frequency of administration and increasing the ocular bioavailability.  Nanolipids were prepared by film hydration technique and then prepared nanolipids were incorporated into insitu gel by using various polymers like Carbopol 940 and HPMC K15M with different concentration. The various formulations prepared showed excellent and effective results for visual appearance, pH, and gellation study. It was further observed that formulations had  entrapment efficiency within the range of 67.20% to 97.3% for brimonidine maleate loaded insitu gel formulations. F1 entrapment efficiency was found to be 97.3% and shown maximum when compared with other formulations. From the drug release data, it was found that F1 (99.0%) shows maximum drug release compare to other formulations.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

Cationic Diclofenac Lipid Nanoemulsion for Improved Oral Bioavailability: Preparation, Characterization and In Vivo Evaluation

2015 ◽  
Vol 8 (2) ◽  
pp. 2874-2880
Author(s):  
Kishan Veerabrahma ◽  
Swapna Madishetty ◽  
Muzammil Afzal Syed ◽  
Prabhakar Kandadi
Keyword(s):  
Oral Bioavailability ◽  
Physical Stability ◽  
Cationic Lipid ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
In Vivo Evaluation ◽  
Drug Content ◽  
Lipid Nanoemulsion

Cationic nanoemulsions were reported to have increased bioavailability. The aim of present study was to prepare a cationic lipid nanoemulsion of diclofenac acid (LNEs) for improved oral bioavailability to treat arthritic conditions. The LNEs of diclofenac acid were prepared by using soya bean oil, egg lecithin, cholesterol and stearylamine. Stearylamine was used as positive charge inducer. The LNEs were processed by homogenization and ultrasonication. The formulation composition was selected based on earlier reports. The LNEs were characterized for size and zeta potential. The physical stability of LNEs was studied using autoclaving, centrifugal, desorption (dilution effect) stresses and on storage. The total drug content and entrapment efficiency were determined using HPLC. During in vivo studies in Wistar rats, the pharmacokinetic parameters of LNEs were compared with a prepared diclofenac suspension in sodium CMC mucilage. The selected formulations, F1, F2 and F3, were relatively stable during centrifugal stress, dilution stress and on storage. The drug content was found to be 2.38 ± 1.70 mg/ml for F1, 2.30 ± 0.82 mg/ml for F2, and 2.45 ± 0.66 mg/ml for F3. The entrapment efficiencies were 97.83 ± 0.53%, 97.87 ± 1.22% and 98.25 ± 0.21% for F1, F2 and F3 respectively. The cumulative percentage drug release from F1, F2 and F3 showed more release in pH 6.8 phosphate buffer than in pH 1.2 HCl. During oral bioavailability studies, the LNEs showed higher serum concentrations than a suspension. The relative bioavailability of the LNE formulations F1, F2 and F3 were found to be 2.35, 2.94 and 6.28 times that of F4 suspension and were statistically significant. Of all, the cationic lipid nanoemulsion (F3) was superior in improving bioavailability, when compared with plain emulsion (F1) and cholesterol containing LNE (F2). The study helps in designing the cationic oral nanoemulsions to improve the oral bioavailability of diclofenac.

Berberine Chloride Dihydrate Enthused Nanovesicles for the Management of Dermatitis

2020 ◽  
Vol 10 ◽  
Author(s):  
Nimisha Srivastava ◽  
Zeeshan Fatima ◽  
Chanchal Deep Kaur ◽  
Dilshad Ali Rizvi
Keyword(s):  
Laser Scanning ◽  
Skin Irritation ◽  
Research Work ◽  
Slight Modification ◽  
Entrapment Efficiency ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Chloride Dihydrate ◽  
E Coli ◽  
Berberine Chloride

Background: Dermatitis is a common inflammatory skin disease that is affecting up to 25% of children and 1%-3% of adults worldwide. Paucity of exact cure for dermatitis and untoward side effects of topical immunosuppressive steroids has resulted into 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.

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