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EVALUATION OF THE EFFECTIVENESS OF USING LIPOSOMAL FORMS OF
VITAMINS, USING VITAMIN C AS THE EXAMPLE
E. R. Tukhvatulina, M. J. Baltaeva
Tashkent Pediatric Medical Institute
Annotation.
Vitamin C is an exogenous compound required for various metabolic processes;
therefore, effective delivery is critical to maintaining div homeostasis. The
pharmacokinetics of vitamin C and its low amounts in processed foods require its
continuous supplementation. In this article, we present a review of a new liposomal vitamin
C formulation free of harmful organic solvents. The formulation was quantitatively
characterized in terms of its chemical composition and nanostructuring. Encapsulation of
vitamins and minerals in liposomes helps improve overall bioavailability.
Key words:
Liposome, pharmacokinetics, bioavailability
Аннотация.
Витамин С является экзогенным соединением, необходимым для
различных метаболических процессов; поэтому эффективная доставка имеет
решающее значение для поддержания гомеостаза организма. Фармакокинетика
витамина С и его низкие количества в обработанных пищевых продуктах требуют его
постоянного добавления. В статье мы представляем обзор на новую липосомальную
формулу витамина С, свободную от вредных органических растворителей. Формула
была количественно охарактеризована с точки зрения ее химического состава и
наноструктурирования. Инкапсуляция витаминов и минералов в липосомы помогает
улучшить общую биодоступность.
Ключевые слова:
Липосома, фармакокинетика,биодоступность.
Annotatsiya.
S vitamini turli metabolik jarayonlar uchun zarur bo'lgan ekzogen birikma;
shuning uchun samarali etkazib berish tananing gomeostazini saqlab qolish uchun juda
muhimdir. S vitaminining farmakokinetikasi va qayta ishlangan oziq-ovqatlardagi past
darajalari uni muntazam ravishda qo'shishni talab qiladi. Ushbu maqolada biz zararli organik
erituvchilardan xoli C vitaminining yangi liposomal formulasini ko'rib chiqamiz. Formula
kimyoviy tarkibi va nanostrukturasi bo'yicha miqdoriy jihatdan tavsiflangan.
Liposomalardagi vitaminlar va minerallarni kapsulalash umumiy bioavailabilityni
yaxshilashga yordam beradi.
Kalit so'zlar:
lipozoma, farmakokinetika.
Today, the creation of new groups of drugs with improved pharmacokinetic properties is an
important area of modern medicine. One of the areas of modern pharmacology is the
method of drug delivery and their bioavailability. This article provides an overview of
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vitamin C in liposomal form, its delivery to organs and tissues, as well as possible side risks
of using this form of vitamin.
Vitamin C is an important antioxidant, it protects organs and tissues from damage caused by
free radicals by activating the div's defenses, enhances and accelerates the repair of
wounds and scars. Vitamin C is a vital vitamin because it participates in the synthesis of
hyaluronic acid, collagen and elastin, is a cofactor of minerals such as calcium, zinc, and
also affects the synthesis of cholesterol. Vitamin C accelerates protein and carbohydrate
metabolism. It is a powerful detoxifier, accelerating the removal of toxic substances from
the div: lead, copper, mercury, vanadium. Vitamin C participates in detoxification
processes in hepatocytes with the participation of cytochrome P 450. The vitamin
participates in the synthesis of interferon, having a direct effect on immunomodulation
processes. Vitamin C is also a cofactor in iron absorption, improving the absorption of iron
from food by converting the Fe3+ ion to Fe2+ with the formation of a complex compound.
Research is currently underway to determine the neuroprotective effects of ascorbic acid in
Alzheimer's disease and the prevention of age-related cognitive decline. However, avoiding
vitamin deficiency appears to have a more beneficial effect than taking large doses as
supplements to a healthy diet. Vitamin C plays an important role in strengthening blood
vessels, increasing the div's endurance, enhancing exercise tolerance. In plasma, it
increases endothelium-dependent vasodilation and reduces extracellular oxidants from
neutrophils. Vitamin C deficiency leads to the potentially fatal disease scurvy, a low
immunity that can only be cured by taking the correct dose of vitamin C. Vitamin C is not
synthesized or accumulated in the div, so it must be replenished regularly. Conventional
forms of ascorbic acid are not fully absorbed, are quickly destroyed, and irritate the
gastrointestinal mucosa. The main advantages of vitamin C enclosed in a liposomal shell are
high bioavailability and protection of the digestive tract mucosa from irritation even when
taking high doses. The liposomal shell consists of phospholipids, which serve as additional
building material for damaged cell membranes.
Vitamin C contained in food or dietary supplements is broken down in the stomach. But the
highly acidic environment of hydrochloric acid can partially neutralize it. To help vitamin C
survive in an acidic environment, its water-soluble molecule is encapsulated in a liposome.
This fat capsule forms a protective shield around vitamin C, protecting it from acid and
transporting it to the small intestine for further absorption. Since most fat digestion occurs in
the small intestine, vitamin C is released there after enzymes from the gallbladder and
pancreas help break down lipids. Liposomes are vesicles that simply mimic the highly
complex cell membranes comprising lipid bilayers surrounding an aqueous core, which have
attracted considerable attention for the delivery and protection of both hydrophilic and
hydrophobic compounds such as vitamins due to their unique properties of biocompatibility
and biodegradability. Accordingly, liposomes can promote the protection and activity of
vitamin C.
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Only a few studies have been published showing the effect of liposomal encapsulation on
the bioavailability of vitamin C. Hickey et al. (Citation2008) found in a very small study
involving only two subjects that the bioavailability of liposomal vitamin C was no different
from that of a 5 gram vitamin C tablet. However, in liposomal vitamin C consisting of
higher dosages such as 20 and 36 g, plasma vitamin C levels resulted in higher plasma levels
than ever previously shown in the literature. This result indicates that liposomes may be an
excellent carrier of vitamin C to achieve higher blood levels of vitamin C that cannot be
achieved with other dosage forms. Davis et al. (Citation2016) assessed plasma levels of oral,
intravenous, and oral liposomal vitamin C. The results showed that liposomal vitamin C has
increased bioavailability than non-liposomal vitamin C while avoiding the risks associated
with intravenous administration (Davis et al. Citation2016). However, no real-world
bioavailability studies have been published for the absorption of liposomal vitamin C (Davis
et al. Citation2016). In 2019, a single-blind study was conducted that measured plasma
vitamin C levels in two subjects in samples taken every half hour or every hour for 6 hours
after vitamin C ingestion. The data were compared with published results and with 10 years
of laboratory plasma determinations. Subjects took 1 gram vitamin C tablets; liposomal
vitamin C. Plasma levels were analyzed using the Butts and Mulvihill method. Preliminary
studies of the effects of liposomal and standard ascorbate have concluded that repeated
doses can maintain levels well above the previously estimated maximum. These findings
have implications for the use of ascorbate as a nutrient and as a drug. With frequent oral
administration, equivalent plasma levels can be maintained indefinitely. Thus, oral vitamin
C has the potential to be used as a non-toxic, sustainable therapeutic agent. A 2021 study
was conducted with the primary objective of evaluating the comparative kinetics of vitamin
C accumulation in leukocytes over 32 hours following acute administration of 250 mg or
500 mg from the two sources. Secondary objectives were to evaluate neutrophil phagocytic
function and lymphocyte differentiation between the two vitamin C sources. Ninety-three
healthy women (250 mg, n = 27; 500 mg, n = 24) and men (250 mg, n = 19; 500 mg, n = 23)
were assigned to receive a single dose of CA or AA providing 250 mg or 500 mg vitamin C
in two separate, double-blind, randomized, crossover trials. Study results revealed no
significant differences in the primary or secondary outcomes between the two treatments in
the low-dose 250 mg trial. In contrast, there was evidence that 500 mg CA increased plasma
docosahexaenoic acid levels, increasing neutrophil functionality during the first 8 hours of
the study. These results suggest that 500 mg CA may provide some immune benefits
compared to 500 mg AA.
A review of the literature has shown that vitamin C may have beneficial effects on blood
pressure, infections, bronchospasm, atrial fibrillation, and acute kidney injury. However, the
practical significance of these effects is unclear. A review of meta-analysis data assessed the
effect of vitamin C on the practical outcomes of intensive care unit (ICU) length of stay and
duration of mechanical ventilation. Eighteen controlled trials with a total of 2004 patients
were analyzed, 13 of which studied patients undergoing elective heart surgery. The analysis
of the data showed that in 12 trials with 1766 patients, vitamin C reduced the length of ICU
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stay by an average of 7.8%. In six trials, oral liposomal vitamin C at doses of 1-3 g/day
(weighted mean 2.0 g/day) reduced the length of ICU stay by 8.6%. The effect of vitamin C
on ICU patients should be studied in more detail. In conclusion, it should be noted that the
inability to produce endogenous vitamin C and uncertain dietary intake can lead to a
deficiency that can be easily corrected by effective supplementation. Most of the vitamin C
in the human div is found intracellularly (over 97%), while only a small portion is found in
extracellular fluids. A complex system of ascorbic acid fluxes in the human div prevents
excessive fluctuations in its intracellular concentrations, as required by metabolic processes.
In order to influence the homeostatic balance using a convenient oral route of delivery,
vitamin C intake must be high enough and preferably spread out over time. To achieve this,
high concentrations of vitamin C in the gastrointestinal tract must be maintained for a long
time so that it is available for absorption and does not require repeated dosing. Maintaining
high levels of vitamin C in the gastrointestinal tract depends mainly on the rate of its
hydrolysis. The degradation of vitamin C can be significantly reduced by its association with
lipid interfaces, which are abundant in the liposomal formulation. This means that if a
certain concentration of ascorbic acid in the digestive tract is maintained for a sufficient
period of time, a high level of absorption will be achieved and maintained. Another
important aspect of the liposomal formulation is the ability to deliver large doses of vitamin
C over a long period of time, since the lipid capsule alleviates the gastrointestinal irritation
that usually accompanies large oral doses of ascorbate. Another important feature of the
presented formula is that the process of liposome formation does not require toxic organic
solvents.
In summary, encapsulation of vitamin C in novel types of liposomes results in enhanced
bioavailability of vitamin C at physiological level without compromising its efficacy at
cellular level. Liposomal vitamin C formulation, in addition to its high activity provided by
enhanced bioavailability, should also satisfy stringent regulatory requirements regarding the
content of potentially harmful compounds, stability and reproducibility of manufacturing
processes. Liposomally encapsulated ascorbic acid (vitamin C) exhibits well-organized
morphological structure, uniform particle size and high efficiency, resulting in enhanced
bioavailability. The structural formation of liposomes makes them a versatile nanocarrier
with the capabilities of loading and delivering multiple drugs/components for specific
disease states. Furthermore, with the advent of combination drug therapy and the
development of new drug products using liposomal formulations, which have shown
significant advantages over traditional drug therapies, there is great potential in this class of
drugs, which can be considered as a preferred drug delivery strategy.
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