scholarly journals Formulation and Evaluation of Liposome by Thin Film Hydration Method

2021 ◽  
Vol 11 (1) ◽  
pp. 72-76
Author(s):  
Mahesh Umbarkar ◽  
Swapnil Thakare ◽  
Tanaji Surushe ◽  
Amol Giri ◽  
Vaibhav Chopade

Liposomes are the most advance formulation for targeting and controlled drug delivery system. These liposomes are generally administered by intra-venous route. In this work the liposome was prepared by using thin film hydration method. The formulated liposome is evaluated or characterised by using zeta sizer, Encapsulation efficiency, Entrapment efficiency, In vitro drug release. Main things are drug which are used for formulation of liposome was Diclofenac sodium, it having anti-inflammatory and anti-pyretic effect. The Diclofenac sodium having several adverse effects, such as depression of renal function, Liver failure for repeated administration, Local mucosal irritation, gastritis. To avoid this adverse effect Diclofenac sodium are incorporate in liposomal formulation. By formulating liposomal formulation, the bioavailability of Diclofenac sodium increase. In conventional dosage form bioavailability of diclofenac sodium is 50℅. But in liposomal formulation bioavailability of this drug increase. The final result includes that diclofenac liposome formulation shows more sustained and prolong anti-inflammatory activity. Keywords: Diclofenac sodium, Liposome, Anti-inflammatory activity.

Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1853-1863
Author(s):  
Shubhra Rai ◽  
Gopal Rai ◽  
Ashish Budhrani

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.


Author(s):  
K.P. Jaiganesh ◽  
T.J. Jasna ◽  
A.C. Tangavelou

Hugonia mystax L., (Linaceae), is commonly distributed in the thorny scrubs and tropical dry evergreen forests of Tamil Nadu, which has been valued for centuries in traditional system of medicine for the treatment of various ailments. In the present study was an attempt to investigate the phytochemical nature and anti-inflammatory, antimicrobial potential by adopting suitable methods. Phytochemical analysis of Hugonia mystax L., plant extracts revealed the presence of various biochemical compounds such as alkaloids, flavonoids, glycosides, triterpenoids and saponins etc. Since triterpenoids and flavonoids have remarkable anti-inflammatory activity, so our present work aims at evaluating in vitro anti inflammatory activity of Hugonia mystax L., by HRBC membrane stabilization method. The inhibition of hypotonicity induced HRBC membrane lysis was taken as a measure of the anti-inflammatory activity. The percentage of membrane stabilization for ethanolic extracts and Diclofenac sodium were done at different concentrations. The maximum membrane stabilization of Hugonia mystax L., extracts was found to be 94.97 % at a dose of 2000 μg/ml. Therefore, our studies support the isolation and the use of active constituents from Hugonia mystax L., in treating inflammations.


INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 60-62
Author(s):  
M. R Elayaraja Krishnan ◽  
◽  
R. Vijaya Kanth ◽  
S. Muthu Pandi

In our present study, various concentrations of pet ether extract of whole plant of Hyptis suaveolens were prepared and subjected for anti arthritic and anti-inflammatory activity by in vitro methods. The antiarthritic activity was carried out by bovine serum albumin denaturation paradigm. The results showed that the pet ether extract (44.51%) showed excellent arthritic activity when compared to the standard diclofenac sodium (31.44%) at 2000μg/mL. Meanwhile, in the anti-inflammatory paradigm, the same extract (99.10%) showed excellent activity than the standard diclofenac sodium (73.80%) at 2000μg/ mL by restoring the stability of degraded red blood corpuscles. In both the paradigms, increase in concentration of the extract increases the action potential against the methanol degradation of bovine albumin and HRBC.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 87-92
Author(s):  
C Sushmitha ◽  
◽  
M.P. Kusuma ◽  
J Archana

Emulgels (emulsion gels) are a class of biphasic semi-solid formulations, having aqueous and non-aqueous phases, delivering both hydrophilic and lipophilic agents. The main advantage of an emulgel is that lipophilic drugs can be easily formulated as emulgels. Rutin trihydrate is an herbal drug used for topical treatment of inflammation. However, its poor water solubility (0.125 mg/ml) presents a hindrance for its local bioavailability and limits effective anti-inflammatory activity. The aim of the current study was to formulate and optimize rutin trihydrate emulgel to enhance its efficacy and stability. 28 formulations were developed with various types of gelling agents like Carbapol 934 (0.8 and 1% w/v), Xanthum gum (1.5 and 2% w/v), HPMCk15 (2, 2.5 and 3% w/v),HPMC K100 (2, 2.5% w/v), guar gum (1, 1.5 and 2% w/v), badam gum (1% w/v) and using various permeation enhancers like clove oil, eucalyptus oil and oil of orange (10 and12.5% v/v). The optimised formulation (f8) was yellow in colour, homogeneous with good consistency, possessed pH of 6.51±0.04 that is very close to that of normal skin (6-7), drug content of 98.7%, viscosity of 14,680cps at 30rpm, spreadability 13.5gm.cm/sec and extrudability 36.2% and in vitro drug release of 79.3% for 7 hrs, ex vivo drug release of 70.08% was stable for 3 months and was having comparable anti inflammatory activity with that of marketed formulation.


2012 ◽  
Vol 02 (02) ◽  
pp. 36-40
Author(s):  
Narayana Charyulu R. ◽  
Gandhi Kinjal B. ◽  
Jobin Jose ◽  
Sneh Priya ◽  
Shastry C. S.

AbstractThe aim of present study was to prepare sustained release formulations of niosomes of methotrexate (MTX) alone (N1 to N10) and along withbioenhancers (NB1 to NB9) by thin film hydration technique using span 60 as surfactant,cholesterol as membrane stabilizing agent, curcumin and piperine as bioenhancers and dicetyl phosphate (DCP) as charge inducing agent. All the formulations of niosomeswere characterized on the basis of physical appearance and entrapment efficiency. The invitro releasestudies of optimized formulation of niosomes of MTX alone and along with bioenhancers were performed and compared with pure drug released. The entrapment efficiency of MTX in optimized formulation of niosomes containing MTX along with bioenhancers was found to 56.9% and entrapment efficiency of bioenhancerscurcumin and piperinewas found to be 40.30% and 69.1%respectively. In vitro drug release of optimized formulationsof niosomes of MTX without and with bioenhancers (F3) was found to be 98.89% and 60.97% at the end of 12 h respectively. Results concluded that Niosomes of MTX containing bioenhancers followed sustain release pattern.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Suresh Purohit

Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higherCmaxthan CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile.


Author(s):  
SEHAM M. SHAWKY ◽  
MAHA K. A. KHALIFA ◽  
HEBA A. EASSA

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p<0.001). Conclusion: The developed nanosponge hydrogel is an efficient nanocarrier for improved and controlled topical delivery of LX.


Author(s):  
Swapna Velivela ◽  
Nikunja B Pati ◽  
B. Ravindra Babu

Temozolomide is an anti-cancer drug; it was encapsulated in liposomal intravenous application. To avoid the side effects and to target the drug to the specific site, we have formulated liposomal formulation of Temozolomide. The liposomal were prepared by dried thin film hydration technique using rotary evaporator with drug and Soya phosphatidyl choline as carrier. The prepared liposomes were characterized for size, shape, % entrapment efficiency, in-vitro drug release and physical stability. The evaluated batches showed good physicochemical characteristics. The maximum encapsulation efficiency of Temozolomide was achieved with formulation TMZ 6 with 40.19% and the in-vitro drug release is 64.94%. Based on the results it can be concluded that TMZ 6 was selected as optimized formulation and the optimized formulation Optimized formulation follows zero order release kinetics and follow super case II transport when it applied to Korsmeyer-Pepps model for mechanism of drug release.


Gels ◽  
2021 ◽  
Vol 8 (1) ◽  
pp. 16
Author(s):  
Heba S. Elsewedy ◽  
Nancy S. Younis ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Wafaa E. Soliman

Recent progression in investigational studies aiming to integrate natural products and plant oils in developing new dosage forms that would provide optimal therapeutic effect. Therefore, the aim of the present exploration was to inspect the influence of jojoba oil in boosting the anti-inflammatory effect of colchicine natural product. To our knowledge, there is no formulation comprising colchicine and jojoba oil together to form a niosomal emulgel preparation anticipated for topical application. Colchicine is a natural product extracted from Colchicum autumnale that has been evidenced to show respectable anti-inflammatory activity. Owing to its drawbacks and low therapeutic index, it was preferable to be formulated into topical dosage form. The current study inspected colchicine transdermal delivery by developing niosomal preparation as a potential nanocarrier included into emulgel prepared with jojoba oil. Box Behnken design was constructed to develop 17 niosomal emulgel formulations. The optimized colchicine niosomal emulgel was evaluated for its physical characteristics and in vitro release studies. The in vivo anti-inflammatory activity was estimated via carrageenan-induced rat hind paw edema method. The developed colchicine niosomal preparation revealed particle size of 220.7 nm with PDI value 0.22, entrapment efficiency 65.3%. The formulation was found to be stable showing no significant difference in particle size and entrapment efficiency up on storage at 4 °C and 25 °C for 3 months. The optimized colchicine niosomal emulgel exhibited a pH value 6.73, viscosity 4598 cP, and spreadability 38.3 mm. In vitro release study of colchicine from niosomal emulgel formulation was around 52.4% over 6 h. Apparently, the proficient anti-inflammatory activity of colchicine niosomal emulgel was confirmed via carrageenan-induced rat hind paw edema test. Overall, the results recommend the combination of niosomal preparation with jojoba oil-based emulgel that might signify a favorable delivery of anti-inflammatory drug such as colchicine.


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