scholarly journals FORMULATION AND EVALUATION OF ELASTIC LIPOSOMES OF DECITABINE PREPARED BY ROTARY EVAPORATION METHOD

2019 ◽  
Author(s):  
Nwobodo Ndubuisi Nwobodo ◽  
Adamude Fatima Amin ◽  
Dingwoke Emeka John ◽  
Abraham Ubhenin
Keyword(s):  
Drug Release ◽  
Dna Methyltransferase ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Topical Administration ◽  
Systemic Circulation ◽  
Stability Study ◽  
Evaporation Method ◽  
Rotary Evaporation

Decitabine is a cytidine deoxynucleoside analog, which acts by inhibiting DNA methyltransferase, and is used for the treatment of acute myeloid leukemia. Decitabine has a short half-life (25 minutes), and is sensitive to harsh conditions. Elastic liposomes are an effective tool that can be used to overcome this disadvantage. Elastic liposomes also known as transfersomes are modified lipid carriers that enable drug to reach deeper skin layers and/or the systemic circulation. These vesicular formulations are several orders of magnitudes, more deformable than the standard liposomes and thus well suited for skin penetration. The objective of present study is to develop and evaluate the elastic liposomes of Decitabine so as to provide the sustained release and improve its bioavailability. Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared Elastic liposomes were evaluated for entrapment efficiency, vesicle size, in vitro drug release. The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. Based on different parameters formulations of batch ELS1 was found to be the best formulations. Stability study was performed on the selected formulation ELS1. Study concludes that Decitabine can also be formulated in the liposomal carrier which finds its best way for the topical administration.

scholarly journals Development and Characterization of Elastic Liposomes of Metronidazole for the Treatment of Bacterial Infection

2020 ◽  
Vol 10 (6-s) ◽  
pp. 83-88
Author(s):  
Priyam Chaurasiya ◽  
Ritesh Agarwal ◽  
Kavita R. Loksh
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Stability Study ◽  
Vesicle Size ◽  
Rotary Evaporation ◽  
Span 60

Objective: The objective of present study is to develop and evaluate the elastic liposomes of metronidazole so as to provide the sustained release and improve its bioavailability. Methods: Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared elastic liposomes were evaluated for entrapment efficiency, vesicle size, In vitro drug release. Results: The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. The formulation prepared showed an average vesicle size 185.4nm. The amount of drug entrapped into the elastic liposomes formulations was determined. The entrapment efficiency was found to be 73.45±0.78 %. A good amount of drug was entrapped in the liposome formulations prepared. Based on different parameters formulations of batch TG2 was found to be the best formulations. Stability study was performed on the selected formulation TG2. When the regression coefficient values of were compared, it was observed that ‘r’ values of first order was maximum i.e. 0.993 hence indicating drug release from formulations was found to follow Korsmeyer Peppas model release kinetics Conclusion: These results indicate that elastic liposome can function as probable drug delivery systems to enhance transdermal permeation of metronidazole for treating the topical infections. Keywords: Metronidazole, Elastic liposomes, Topical administration, Skin infection

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

scholarly journals Formulation Development and Evaluation of Sustained Release Microsphere of Levetiracetam

2021 ◽  
Vol 71 (2) ◽  
Author(s):  
Dinesh V. Panpaliya ◽  
Atish Y. Sahare ◽  
Priyanka Lanje ◽  
Pooja Dhoke
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Solvent Evaporation Method ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Evaporation Method

The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity

FORMULATION AND EVALUATION OF ACECLOFENAC NIOSOMES BY USING MIXTURE OF SURFACTANTS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 21-26
Author(s):  
C.H. Sravanthi ◽  
◽  
S. Punitha
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Therapeutic Index ◽  
Reverse Phase ◽  
Evaporation Method ◽  
Zero Order Kinetics ◽  
Reduced Toxicity ◽  
Span 60

The present study was aimed at the overall improvement in the efficacy, reduced toxicity andenhancement of therapeutic index of aceclofenac. Niosomal delivery system of aceclofenac has beendeveloped by various techniques using mixture of Span 60/40 (surfactant) along with cholesterol in1:1 ratio. The formulations were then characterized with respect to vesicle diameter, drug content,entrapment efficiency, in-vitro drug release and release kinetics. The formulated aceclofenac niosomeswere discrete and round in shape. The lowest entrapment efficiency was found to be 75% (F2) andwas highest in reverse phase evaporation method 95% (F5). Percentage cumulative drug release waswell retarded for up to 24 h in F5 (59%) compared to all other formulations and its release pattern wasanalysed by using various mathematical models and found to follow under zero order kinetics. From thet50% values of F5, it is concluded that the reverse phase evaporation method seems to extend the drugrelease for prolonged period.

scholarly journals EFFECT PROCESSING VARIABLES ON THE CHARACTERISTICS OF ITRACONAZOLE HOLLOW MICROSPHERES

2019 ◽  
pp. 108-115
Author(s):  
SURBHI ROHILLA ◽  
D. C. BHATT ◽  
SHAVETA AHALWAT
Keyword(s):  
Drug Release ◽  
Spherical Surface ◽  
Entrapment Efficiency ◽  
Storage Conditions ◽  
Physicochemical Analysis ◽  
Stability Study ◽  
Hollow Microspheres ◽  
Release Mechanism ◽  
Low Density

Objective: The purpose of the study was to develop the multiple unit non-effervescent gastroretentive floating hollow microspheres to enhance the bioavailability of the drug by varying the concentration of low-density polymer and release modifier to retaining the formulation at its absorption site. Design of experiment approach applied to get the best possible formulation with minimum assets and experimentation. Methods: The hollow microspheres were prepared by emulsion solvent diffusion-evaporation technique using ethylcellulose as low-density polymer and Eudragit E100 as release modifier. The central composite design was used for the optimization of independent variables and was evaluated for particle size, entrapment efficiency, in vitro floating ability and drug release characteristics. Results: The physicochemical analysis was done to confirm any interaction between drug and excipients. The Scanning Electron Microscopy (SEM) showed a smooth, spherical surface with an inner hollow cavity. The stability study proves that the hollow microspheres were more stable under different storage conditions with no significant changes in formulation. The drug release mechanism of the optimized batch can be explained by Korsmeyer Peppas model. Conclusion: Based on the results, the hollow microspheres with a release modifying polymer offers a superior approach to retain the formulation in the stomach.

scholarly journals Formulation and In Vitro Penetration Study of Recombinant Human Epidermal Growth Factor-Loaded Transfersomal Emulgel

2020 ◽  
Vol 10 (4) ◽  
pp. 586-594 ◽  
Author(s):  
Silvia Surini ◽  
Astried Leonyza ◽  
Chang Woo Suh
Keyword(s):  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Molecular Size ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Stability Study ◽  
Lipid Vesicle ◽  
Human Epidermal Growth Factor ◽  
Epidermal Growth

Purpose : Recombinant human epidermal growth factor (rhEGF) is a 6045-Da peptide that promotes the cell growth process, and it is also used for cosmetic purposes as an anti-aging compound. However, its penetration into skin is limited by its large molecular size. This study aimed to prepare rhEGF-loaded transfersomal emulgel with enhanced skin penetration compared with that of non-transfersomal rhEGF emulgel. Methods: Three transfersome formulations were prepared with different ratios between the lipid vesicle (phospholipid and surfactant) and rhEGF (200:1, 133:1, and 100:1) using a thin-film hydration-extrusion method. The physicochemical properties of these transfersomes and the percutaneous delivery of the transfersomal emulgel were evaluated. Long-term and accelerated stability studies were also conducted. Results: The 200:1 ratio of lipid to drug was optimal for rhEGF-loaded transfersomes, which had a particle size of 128.1 ± 0.66 nm, polydispersity index of 0.109 ± 0.004, zeta potential of −43.1 ± 1.07 mV, deformability index of 1.254 ± 0.02, and entrapment efficiency of 97.77% ± 0.09%. Transmission electron microscopy revealed that the transfersomes had spherical and unilamellar vesicles. The skin penetration of rhEGF was enhanced by as much as 5.56 fold by transfersomal emulgel compared with that of non-transfersomal emulgel. The stability study illustrated that the rhEGF levels after 3 months were 84.96–105.73 and 54.45%–66.13% at storage conditions of 2°C–8°C and 25°C ± 2°C/RH 60% ± 5%, respectively. Conclusion: The emulgel preparation containing transfersomes enhanced rhEGF penetration into the skin, and skin penetration was improved by increasing the lipid content.

scholarly journals DEVELOPMENT AND IN VITRO EVALUATION OF PHYTOSOMES OF NARINGIN

2019 ◽  
pp. 252-256
Author(s):  
JEEVANA JYOTHI B ◽  
MARY RAGALATHA P
Keyword(s):  
Oral Absorption ◽  
Therapeutic Potential ◽  
Entrapment Efficiency ◽  
Precipitation Method ◽  
Therapeutic Effects ◽  
Evaporation Method ◽  
Rotary Evaporation ◽  
Soya Lecithin ◽  
Antisolvent Precipitation

Objective: Phytosomes are novel herbal formulations meant for design of poorly soluble flavonoids of therapeutic potential. Naringin is a flavanone with poor oral absorption and bioavailability but possess antioxidant, anti-inflammatory, antiapoptotic, anti-ulcer, antiosteoporotic, and anticarcinogenic effects. Hence, the objective of the present work is the development of phytosomes of naringin to enhance its dissolution so that its therapeutic effects can be exploited. Materials and Methods: Phytosomes containing 350 mg of naringin were prepared by antisolvent precipitation method and rotary evaporation method using soya lecithin as main polymer. The prepared phytosomes were evaluated by entrapment efficiency, in vitro drug release studies, and drug-excipient interaction studies. Results: Phytosomes made by rotary evaporation method evidenced higher dissolution values than phytosomes made by antisolvent precipitation. Formulation F7 containing 350 mg of naringin and 1400 mg of soya lecithin revealed the highest percentage release of 84.5±0.39% in 60 min and 99.7±0.24% in 120 min. The percentage of drug entrapment efficiency values was satisfactory. Fourier-transform infrared spectroscopy spectra of pure naringin and naringin phytosomes revealed no interaction between the drug and polymers used for preparation. Conclusion: Naringin phytosomes are produced successfully by the rotary evaporation method. Phytosomes made with 350 mg of naringin and 1400 mg of soya lecithin by rotary evaporation method are spherical with a rough outer surface and optimum release characteristics of 84.5±0.39 in 60 min to possess optimum bioavailability and 99.7% in 120 min.

scholarly journals Formulation and in-vitro evaluation of Glipizide (Anti diabetic drug) Liposphere

2018 ◽  
Vol 8 (6-s) ◽  
pp. 116-119
Author(s):  
Sarika Saini ◽  
Aman Mittal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Paraffin Wax ◽  
Drug Content ◽  
Dissolution Apparatus ◽  
Dispersion Technique

Objective- The aim of the present study was to formulate and in- vitro study of glipizide liposphere by using melt dispersion technique. Methods- Glipizide Liposphere system composed of paraffin wax, Stearic acid as lipid phase and sodium lauryl sulphate as surfactant. Glipizide lipospheres were prepared by using melt dispersion technique. Formulation of Glipizide was evaluated such as organoleptic properties, particle size, drug content, entrapment efficiency in-vitro study and stability of the lipospheres. Result- The formation of glipizide lipospheres by using melt dispersion technique was done successfully. All the formulations have off- white in colour, characteristic odour and spherical shape. The formulation A4 has particle size 19.65 μm, drug content 84.93 %, entrapment efficiency 80.75 % and the percentage drug release was carried out by using USP type 2 dissolution apparatus in 6.8 pH phosphate buffer solution and drug release of glipizide lipospheres within 12 hrs was found to be 74.06 %.stability study of glipizide lipospheres revealed that the formulation was stable at 5oC ± 3oC. Keywords- Lipospheres, Glipizide, Paraffin wax, Melt dispersion method, Dissolution Apparatus, Stability study

scholarly journals Development and Evaluation of Novel Bionanoparticles Loaded with Nanosized Lamotrigine by Using the Novel Isolated Biopolymer from Phaseolus vulgaris Seeds

2020 ◽  
pp. 247-254
Author(s):  
Sushant Kumar ◽  
Nookala Venkala Satheesh Madhav ◽  
Anurag Verma ◽  
Kamla Pathak
Keyword(s):  
Particle Size ◽  
Phaseolus Vulgaris ◽  
Drug Release ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Term Treatment ◽  
Stability Study ◽  
The Novel ◽  
Long Term Treatment

The aim of this research was to isolate and characterize the novel biopolymer from Phaseolus vulgaris seeds and to formulate lamotrigine loaded bionanoparticles using this biomaterial. The biopolymer was isolated by simplified and economical process and analysed for different physico-chemical and spectral properties. The nanosizing of lamotrigine was done by bath sonication method and its particle size in nano-range was screened by UV method. The bionanosuspension loaded with nanosized lamotrigine was prepared by bath sonication for 15 cycles (1cycle equal to 3 minutes). The formulated bionanosuspension loaded with lamotrigine using biopolymer was compared with lamotrigine loaded bionanosuspension by using HPMC.  The bionanosuspension was subjected for pH study, dispersibility study, % entrapment efficiency, nanosizing screening, particle size study and in vitro study for drug release and stability study of formulated bionanosuspension. The best formulation LPVu7 showed up to 90.36 ±0.9% drug release in 36 hours. having t 50% of 17 hours and t80% of  29 hours with r2 value of 0.9927 as compared to release from LSP5 with 92.43±0.68%   having t 50% of 16 hours and t80% of  28 hours with r2 value of 0.9951 in  36 hours. The results reveal that isolated biopolymer may be used as an alternative to synthetic polymer because of its novel inbuilt bioretardant cum biostabilizing properties. The formulated bionanosuspension are feasible for delivering the nanosized lamotrigine in sustained manner for prolonged time for long term treatment of epilepsy.

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