Ultradeformable vesicles: concepts and applications relating to the delivery of skin cosmetics

Skin aging is a phenomenon resulting in reduced self-confidence, thus becoming a major factor in social determinants of health. The use of active cosmetic ingredients can help prevent skin aging. Transfersomes are well known to be capable of deeply penetrating the dermis. This scoping review provides an insight into transfersomes and their prospective use in anti-aging cosmetics. Numerous reports exist highlighting the successful skin delivery of therapeutic agents such as high-molecular-weight, poorly water soluble and poorly permeable active ingredients by means of transfersomes. Moreover, in vitro and in vivo studies have indicated that transfersomes increase the deposition, penetration and efficacy of active ingredients. However, the use of transfersomes in the delivery of active cosmetic ingredients is limited. Considering their similar physicochemical properties, transfersomes should possess considerable potential as a delivery system for anti-aging cosmetics

Development and Validation of Spectrophotometry UV-Vis Method for Determination of Primaquine and Chloroquine in Liposome Dosage Form

Development and validation of UV-Vis Spectrophotometry method for simultaneous determination of primaquine and chloroquine in liposome dosage form has been carried out. The method was tested for selectivity, linearity, accuracy, and precision. A phosphate buffer solution pH 7.4 was used as a solvent and observations were made at wavelengths of 220 and 260 nm for simultaneous equations method. The selectivity results of primaquine and chloroquine showed no interference from liposome. Linearity result (r value) of the simultaneous equation method was 0.9998 with the value of Vxo less than 0.5% for both primaquine and chloroquine in the concentration range of 2–10 mg/L. Accuracy was done using spiked placebo method and obtained data analyzed using simultaneous equation method. Persentage recovery of primaquine was 89–97% and 79–108% for chloroquine. The intra-and interday precision of primaquine were 1.72 and 2.57%, respectively. Whereas the intra-and interday precision of chloroquine were 6.93 and 8.77, respectively. Further observation using chromatography method need to be done to have better accuracy results for both substances

Transdermal patch loading diclofenac sodium for anti inflammation therapy using rat paw oedema model

The anti-inflammatory effect of transdermal delivery of a diclofenac sodium patch was evaluated. The patch matrix consists of ethyl cellulose N-20 and polyvinyl pyrrolidone K-30 to control the drug release. In this study, the patches were prepared with ethyl cellulose N-20 (EC-N20) and polyvinylpyrrolidone K-30 (PVP K-30) at weight ratio of 6:4 and 7:3 for EC/PVP-6/4 and EC/PVP-7/3 patches, respectively. The anti-inflammatory effect was determined by evaluating the swelling of rat’s paw oedema that was induced with 1% carrageenan suspension. The results showed that the high concentration of PVP K-30 resulted in less rigid patch with pore structures. In addition, it improved the antiinflammatory effect of diclofenac sodium resulted in higher efficacy of EC/PVP-6/4 than that of EC/PVP-7/3. There were no significant differences on drug stability observed for both formulations. It can be concluded that controlling diclofenac sodium released from patch using PVP K-30 could give benefits for anti-inflammation therapy

Characterization and in vitro release study of artesunateloaded microparticles prepared using crosslinked-chitosan and its derivatives

Purpose: To determine the effect of crosslinking on the physical characteristics, recovery, and release of artesunate-loaded chitosan and carboxymethyl chitosan microparticles.Methods: The artesunate microparticles were prepared by means of ionic gelation-spray drying methods involving the use of a crosslinking agent i.e. tripolyphosphate for chitosan and CaCl2 for carboxymethyl chitosan. The drug-polymer solution mixture was introduced into the crosslinker solution and stirred for two hours at 500 rpm prior to drying at a temperature of 100ºC, a pressure of 2 mbar and a flow speed of 6.0 mL/min. The resulting microparticles were subsequently evaluated for their morphology, physical state, drug content and in vitro drug release.Results: The results showed that the type of chitosan and crosslinking affected particle shape, surface roughness, drug recovery, and drug release. The artesunate microparticles prepared with cross-linked polymer demonstrated a lower encapsulation efficiency due to the barriers presented by the crosslinking agents. The use of carboxymethyl chitosan increased the release rate of the artesunate from the microparticles by up to 1.2 times (16.78 mg/ml.min½), while chitosan decreased it 0.7 times (9.12 mg/ml.min½) compared to artesunate alone (13.54 mg/ml.min½).Conclusion: The use of crosslinking agents and chitosan type affects the physical characteristics of artesunate in addition to its release rate from microparticles. Keywords: Artesunate, Chitosan, Carboxymethyl chitosan, Crosslinking, Microparticle, Drug releas

Improving the anti-ageing activity of coenzyme Q10 through protransfersome-loaded emulgel

Coenzyme Q10 (CoQ10) is a naturally produced organic molecule which acts as an antioxidant agent, including in skin anti-ageing, and plays a major role in the social determinants of health. However, its level in the body will decrease during ageing. Therefore, an external supplement is required to repair damaged skin, especially the skin dermis layer. This study aims to evaluate the use of a protransfersomal emulgel to improve the skin delivery and stability of CoQ10 which demonstrates low water solubility, poor permeability and instability. CoQ10 was initially dissolved in oleic acid at a weight ratio of 1:56. Protransfersome was then loaded with CoQ10 (Protransf-CoQ10) and prepared using a composition of L-α-Phosphatidylcholine and Tween 80 at a molar ratio of 85:15. The Protransf-CoQ10 was dispersed in an emulgel base consisting of Tween 80 and Span 80 to produce Protransf-CoQ10 emulgel. The in vivo studies of anti-aging activity and irritability were further evaluated by applying daily 200 mg of emulgels twice a day to a 4 cm2 section on the back of a UV-ray aging-induced male Balb/c mouse 20 min before irradiation. The results showed that Protransf-CoQ10 could transform into transfersomal vesicles with particle sizes of approximately 201.5 ± 6.1 nm and a zeta potential of − 11.26 ± 5.14 mV. The dispersion of Protransf-CoQ10 into emulgel base resulted in stable Protransf-CoQ10 Emulgel during 28 days of observation at low temperatures. Moreover, the in vivo study revealed that Protransf-CoQ10 Emulgel successfully increases the collagen density and number of fibroblast cells in UV radiation skin-aged induced-mice which reflects its potential for repairing the skin ageing process. In addition, the 24-h topical application of Protransf-CoQ10 Emulgel showed that no erythema or skin rash was observed during the study. In conclusion, loading CoQ10 into protransfersomal Emulgel successfully enhanced the stability and anti-ageing efficacy enabling its potential use as anti-ageing cosmetics

Enhancing skin penetration of epigallocatechin gallate by modifying partition coefficient using reverse micelle method

Aim: (-)-Epigallocatechin gallate (EGCG) has been reported as inducing apoptosis in cervical cancer. However, EGCG demonstrates low skin permeability. In order to develop topical delivery of EGCG, the partition coefficient, log P, was modified using a reverse micelle method. Results & methodology: During this study, Tween 80 and Span 80 were added to EGCG at hydrophilic-lipophilic balance (HLB) values of 4.3, 6 and 8. The results showed that lowering the HLB value increases the log P value of EGCG and results in higher IC50 values in Henrietta Lacks (HeLa) cancer cells than that of EGCG. Surfactant-modified EGCG-HLB 6 produced faster and deeper skin penetration than EGCG. Conclusion: Modification of log P value using a combination of Tween 80 and Span 80 improved cytotoxicity and topical delivery of EGCG

Dual Loading Of Primaquine And Chloroquine Into Liposome

Primaquine (PQ) has long been recognized as the only effective drug in the treatment of hepatic stage malaria. However, severe toxicity limits its therapeutical application. Combining PQ with chloroquine (CQ) has been reported as enhancing the former’s efficacy, while simultaneously reducing its toxicity. In this study, the optimal conditions for encapsulating PQ-CQ in liposome, including incubation time, temperature and drug to lipid ratio, were identified. Furthermore, the effect of the loading combination of these two drugs on liposomal characteristics and the drug released from liposome was evaluated. Liposome is composed of HSPC, cholesterol and DSPE-mPEG2000 at a molar ratio of 55:40:5 and the drugs were loaded by means of the transmembrane pH gradient method. The particle size, ζ-potential and drug encapsulation efficiency were subsequently evaluated. The results showed that all liposome was produced with a similar particle size and ζ-potential. PQ and CQ could be optimally loaded into liposome by incubating the mixtures at 60oC for 20 minutes at a respective drug to lipid ratio of 1:3 for PQ and CQ. However,compared to single drug loading, dual-loading of PQ+CQ into liposome resulted in lower drug encapsulation and slower drug release. In conclusion, PQ and CQ can be jointly loaded into liposome with differing profiles of encapsulation and drug release

The Development of tablet formulation of Artocarpus champeden Stembark extract as antimalarial drug

Parasite resistance to antimalarial drug, chloroquine and sulfadoxin-pirimetamin, still e major problem in malaria control worldwide, thereforc, the cffort in developing a new targct of antimalarial drug become a high priority. Our preliminary test revealed that fuom A. chanpeden exhibiedt potent antimalarial activities againts P. lalciparum in vitro brghci in vivo. Several isolaEd compounds from this plant exhibited antimalarial activity drc isotated compound identified as hetcroflavon C, a prenylated flavooe, have a higher activity than chloroquine. Therefore, it is potential to be developed as antimalarial rcscarch was conducted to develop tablet formulation of ethanol extract of A. stcmbark (EEAC). The formula that composed: EEAC 150 mg, lactose 140 mg, cabarnilum 46 mg, avicel PH l0l 79o, primogcl 57o, and Mg stcarat 1% was the selected Th€ tablet hardness o[ the formula has span betwccn 9.0-12.27 kP and the averagc is , thc disintegration time of formula 12 minutcs 4? seconds. A standard fiays test oll P. infected mice was used to evaluated in vrv, antimalarial activity of the tablet. This rlvcalcd that EEAC tablet has antimalarial activity against parasite P. berghei in vivo. ration ofEEAC tablet at a dose of 10 mg/kg body weight multiple dose (twice a day) thc parasite growth better than 100 mg/kg body weight single dose (once a day) activity of tablet in multiple dose pcr oral shqwed inhibition of parasite growth of while at single dose per oral showed inhibition of parasite growth of 83.32

Characterization and Stability Study of Amniotic Membrane Stem Cell Metabolite Product (AMSC-MP)

The purpose of this study was to determine the characteristic and stability of Amniotic Membrane Stem Cell Metabolite Product (AMSC-MP) in fluid and freeze dried form. Conducted a qualitative test of the liquid and freeze dried AMSC-MP form using the SDSPAGE method, also determined the quantitative TGF-β levels, stability stored testing both materials at room and cold temperature during 28 days. Characterization of the freeze dried form was also carried out including FTIR profile, DTA, SEM and XRD.SDS-PAGE results obtained that qualitatively the liquid and freeze dried forms have the same protein component a molecule weight (MW) of 75.33 kDa. Quantitatively, the form of fluid has higher TGF-β levels compared to freeze dried on day 0. However, the results of the stability test showed that the form of freeze dried has better stability than the fluid, as indicated by a decrease in TGF-β levels greater on the day 21st. Liquid form that is stored at room temperature changes the color after 7days. Furthermore characterization of freeze dried shows has a crystalline structure based on its XRD profile with an endothermic peak at 163.8 this is supported by SEM a tetragonal crystal. FTIR profile showed the maximum absorption at wave numbers 1674-1640 and 3350-3200 which indicates the presence of C=O and N-H bonds which are functional groups of protein compounds.Conclusion: The freeze dried AMSC-MP form has better stability than the fluid form in cold temperature storage and AMSC-MP is a protein

The effect of surfactant type on characteristics, skin penetration and anti-aging effectiveness of transfersomes containing amniotic mesenchymal stem cells metabolite products in UV-aging induced mice

Transfersome has been developed to enhance dermal delivery of amniotic mesenchymal stem cell metabolite products (AMSC-MP). AMSC-MP contains many growth factors for managing skin aging, thus improving the quality of an adjusted life year. This study aims to determine the effect of surfactant types acting as the edge activator on transfersome-loading AMSC-MP. Transfersome was prepared by thin-layer hydration method and composed of l-α-phosphatidylcholine as a phospholipid and three types of surfactants, namely; cationic (stearylamine), anionic (sodium cholate), and nonionic surfactant (Tween 80) at a weight ratio of 85:15, respectively. Transfersomes were evaluated for physical characteristics, penetration, effectiveness, and safety. The results showed that sodium cholate, an anionic surfactant, produced the smallest transfersome particle size, i.e., 144.2 ± 3.2 nm, among all formulas. Trans-SA containing stearylamine had a positive charge of 41.53 ± 6.03 mV compared to Trans-SC and Trans-TW, whose respective charges were –56.9 ± 0.55 mV and –41.73 ± 0.86 mV. The small particle size and low negative value of zeta potential enabled high dermal penetration by transfersomes containing AMSC-MP, while the positive charge of stearylamine hindered its penetration of deeper skin layers. Trans-SC and Trans-TW produced higher collagen density values at 77.11 ± of 4.15% and 70.05 ± of 6.95%, than that of Trans-SA. All the AMSC-MP transfersomes were relatively safe with 0.5–1.0 macrophage cell numbers invaded the dermis per field of view. In conclusion, sodium cholate, an anionic surfactant, demonstrated considerable capacity as the edge activator of transfersome-loading AMSC-MP for skin anti-aging therapy