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1.
J Adv Pharm Technol Res ; 15(1): 37-42, 2024.
Article in English | MEDLINE | ID: mdl-38389966

ABSTRACT

Lactobacillus casei (LC) is a type of lactic acid bacterium that is known for its beneficial probiotic properties. However, it is not typically found in the human intestine because it lacks acid resistance. LC thrives in an optimal pH environment of 6.8 and can be initiated in a more acidic environment at a pH of 3.5. This study purposed to compare the effect of L-type methacrylic acid copolymer (MAC) as a matrix (0.50%, 0.75%, and 1.00%) on the physical characteristics of LC probiotic microparticles made by the spray drying process. Probiotic microparticles were also made from a dry suspension of LC FNCC 0090 bacteria and dispersed in a solution of L-type MAC. The results showed that a rise in matrix content by 1.00% increased particle size (4.47 ± 0.19 µm) and reduced moisture content (7.45 ± 0.11%). The analysis of microparticle morphology also indicated a positive correlation between the level of L-type MAC and the production of smooth, nonporous, and almost spherical shapes. In addition, it was observed that encapsulation efficiency (92.46 ± 0.17%) and protection against stomach acid (98.17% ±1.17%) increased with the level of the matrix.

2.
Drug Deliv ; 29(1): 3443-3453, 2022 Dec.
Article in English | MEDLINE | ID: mdl-36471900

ABSTRACT

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.


Subject(s)
Mesenchymal Stem Cells , Pulmonary Surfactants , Mice , Animals , Surface-Active Agents/metabolism , Administration, Cutaneous , Sodium Cholate , Drug Carriers/metabolism , Skin/metabolism , Excipients/pharmacology , Pulmonary Surfactants/metabolism , Aging , Liposomes/metabolism
3.
Sci Rep ; 12(1): 906, 2022 01 18.
Article in English | MEDLINE | ID: mdl-35042910

ABSTRACT

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.


Subject(s)
Protein Precursors , Transforming Growth Factor alpha
4.
Ther Deliv ; 12(10): 739-756, 2021 10.
Article in English | MEDLINE | ID: mdl-34519219

ABSTRACT

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.


Subject(s)
Cosmetics , Skin Aging , Prospective Studies , Skin
5.
J Basic Clin Physiol Pharmacol ; 32(4): 517-525, 2021 Jun 25.
Article in English | MEDLINE | ID: mdl-34214318

ABSTRACT

OBJECTIVES: This study aims to develop coenzyme Q10 nanostructured lipid carriers (NLCs) using tristearin and stearyl alcohol as well as isopropyl palmitate (IPP) as solid and liquid lipid respectively for the dermal delivery system. METHODS: The coenzyme Q10 NLCs were optimized using tristearin, and stearyl alcohol in different concentrations and further characterized by dynamic light scattering (DLS) for particle size, polydispersity index (PDI), zeta potential, differential scanning calorimetry (DSC) and X-ray diffractometry for crystallinity behavior, Fourier transform infrared spectroscopy (FT-IR) for drug-lipid interaction, scanning electron microscopy (SEM) for particle shape, viscometer for viscosity, and pH meter for pH value. Furthermore, entrapment efficiency (EE), drug loading (DL), and skin penetration in vivo were also evaluated while molecular docking was conducted to examine the interaction between coenzyme Q10 and the lipids. RESULTS: The coenzyme Q10 NLCs with tristearin-IPP and stearyl alcohol-IPP as lipid matrix had <1,000 nm particle size, <0.3 PDI, less negative than -30 mV zeta potential, about 41% crystallinity index, and about six as the pH value. Moreover, the EE, DL, viscosity, and in vivo skin penetration of the NLCs using tristearin were higher compared to stearyl alcohol, however, the skin penetration depths for both NLCs were not significantly different. Furthermore, the in silico binding energy of coenzyme Q10-tristearin was lower compared to coenzyme Q10-stearyl alcohol. Both of them showed hydrophobic and van der Waals interaction. CONCLUSIONS: The NLCs of coenzyme Q10 were formulated successfully using tristearin-IPP and stearyl alcohol-IPP for dermal delivery.


Subject(s)
Nanostructures , Drug Carriers , Fatty Alcohols , Lipids , Molecular Docking Simulation , Spectroscopy, Fourier Transform Infrared , Triglycerides , Ubiquinone/analogs & derivatives
6.
Article in English | MEDLINE | ID: mdl-31860468

ABSTRACT

Background Coenzyme Q10 is a fat-soluble antioxidant that can help to prevent collagen and elastin damage and avoid wrinkles. Coenzyme Q10 has several disadvantages to be formulated in topical dosage forms, such as low water solubility and large molecular weight. These make coenzyme Q10 retained in the stratum corneum and cause low skin penetration, so proper formulation is required to get products that can penetrate the skin layer. A nanostructured lipid carrier (NLC) consists of a matrix of solid lipids and liquid lipids in a certain amount with nanoparticle size; it may help increase the penetration of active ingredients. Methods For the antiaging activity test, mice were grouped into four treatment groups and killed on the 14th day; then the back of the skin was stained with Masson trichrome staining. For the irritation test, the mice were grouped into three groups and killed after 24 h; then the back of the mice was stained with hematoxylin-eosin staining. Results The number of fibroblasts in mice with NLC coenzyme Q10 is highest from all test groups. The irritation test results after 24 h of application preparation showed that NLC coenzyme Q10 did not irritate the skin of the back of male mice. Conclusions One percent coenzyme Q10 loaded in NLC induced the number of fibroblast cells in the mice model and showed no irritability effect in histopathology preparations.


Subject(s)
Aging/drug effects , Fibroblasts/drug effects , Skin Absorption/drug effects , Skin Irritancy Tests/statistics & numerical data , Skin/drug effects , Ubiquinone/analogs & derivatives , Animals , Cell Count/statistics & numerical data , Drug Carriers/adverse effects , Drug Carriers/pharmacology , Lipids/chemistry , Male , Mice , Nanostructures/adverse effects , Nanostructures/chemistry , Particle Size , Ubiquinone/adverse effects , Ubiquinone/chemistry , Ubiquinone/pharmacology
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