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The new PMC design is here! Learn more about navigating our updated article layout. The PMC legacy view will also be available for a limited time. Federal government websites often end in. The site is secure. It is characterized by inflammation of the hair bulb and the attached sebaceous gland. To date, many strategies have been used to treat acne as a function of the disease severity.
However, common treatments for acne seem to show several side effects, from local irritation to more serious collateral effects. The use of topical vesicular carriers able to deliver active compounds is currently considered as an excellent approach in the treatment of different skin diseases. Many results in the literature have proven that drug delivery systems are useful in overcoming the toxicity induced by common drug therapies, while maintaining their therapeutic efficacy.
Starting from these assumptions, the authors reviewed drug delivery systems already realized for the topical treatment of acne, with a focus on their limitations and advantages over conventional treatment strategies. Although their exact mechanism of permeation is not often completely clear, deformable vesicles seem to be the best solution for obtaining a specific delivery of drugs into the deeper skin layers, with consequent increased local action and minimized collateral effects.
It often persists into adulthood with a negative impact on the quality of life. The face is the most prone to acne skin lesions but the upper back, chest, neck and shoulders can also be affected, and scarring can last for life. The is benzac good for your skin follicle inflammation can result from several causes: 1 excessive sebum secretion from sebaceous glands, 2 hyperkeratinization and follicular plugging, 3 androgen-mediated effects, 4 inflammation and immunological host reactions, and 5 bacterial proliferation within the follicle.
Propionibacterium acnes P. In particular, different research groups have confirmed the correlation between acne vulgaris and psychological suffering, such as anxiety and depression. Acne can be differentiated into three categories, as a function of its clinical manifestations: mild, moderate and severe. In the case of moderate acne onset, more inflammatory lesions, occasional nodules or both appear. Finally, in severe acne, inflammatory lesions, nodules or both are common.
The choice of treatment is generally related to the severity of the disease, and topical treatments are the first choice in mild and moderate acne because they generally have favorable safety profiles, while systemic therapies are preferred in severe and moderate cases.
However, there is currently no definitive cure for acne. Owing to the complex etiopathogenesis of acne, as mentioned in the Introduction, different anti-acne drugs are used to treat the possible pathogenic factors. According to the new acne clinical guidelines of the American Academy of Dermatology, topical treatments based on benzoyl peroxide, retinoids or a combination of topical drugs including antibiotics are the first line treatment options for mild acne disease.
Among these, retinoids present the best comedolytic activity, but they show a moderate anti-inflammatory and antibacterial efficacy. Although topical acne treatment is safer than systemic therapies, and therefore it is considered as first-line therapy for mild and moderate acne, there are both advantages and disadvantages of topical use.
First of all, the application of topical drugs is not free from side effects. The most common cutaneous manifestations are local skin irritation, which looks like erythema, dryness or scaling; in the case of benzoyl peroxide and topical retinoids, the worst irritating effects are shown, and sometimes this leads to the patient discontinuing therapy.
On valor benzac ac other hand, benzoyl peroxide shows advantages owing to its oxidative mechanism, it reduces anaerobic bacteria and is rapidly reduced to benzoic acid, so it is considered safe for use in pregnant or lactating women.
Another advantage of treatment with benzoyl peroxide is that it does not confer P. However, the anti-oxidative defense of the stratum corneum could be compromised by the potent oxidative stress inflicted by the drug. The loss of vitamin E from the epidermal barrier was also reported and could represent a limit of its topical use as a free drug. It is noteworthy that the combination of benzoyl peroxide with tretinoin or adapalene showed an increased activity but, at the same time, increased collateral effects were also reported.
Dryness and burning are less common side effects for topical antibiotics, while drug resistance may occur following a longer treatment with topical antibiotics. In particular, their use in monotherapy can lead to P. So, the association of different topical antibiotics or the combination of antibiotics and benzoyl peroxide is often required.
Azelaic acid is another drug commonly used for acne treatment. It seems to be active in the reduction of bacteria also showing anti-inflammatory effects. Although it may lead to topical effects such as burning and tightness, it is safe in pregnant and benzac notice females because it is a natural compound generally present on the skin, so it normally does not causes systemic side effects. Other topical and increasingly conventional treatments proposed for acne treatment include light therapy and photodynamic therapy.
Individuals with inflammatory acne exhibited beneficial effects if treated with these procedural therapies based on photosensitizers and a light source. However, some data have shown that patients occasionally present with local blisters and pain, and therefore further studies are necessary to prove the safety of this treatment.
Despite the proven efficacy of topical treatments, none of the most frequently prescribed anti-acne drugs are free from side effects. Not only are collateral effects due to the dose of drug administered, but they also seem to be related to the type of formulation used. In addition to the several side effects which can occur following a topical administration of anti-acne drugs, an important limitation is the inability of many drugs in free form to cross the stratum corneum.
The stratum corneum represents the main skin barrier, and it reduces the efficacy of the topical treatment of different diseases, hindering drug permeation through the skin. Moreover, they provide good therapeutic efficacy of the carried drug, increasing its local efficacy and also minimizing its side effects.
In one study, transepidermal water loss TEWLthe main indicator of skin barrier integrity, was monitored in vitro after the topical application of niosomes, etho and ultradeformable vesicles, and an initial alteration of values was observed, owing to the interaction between carrier and membrane, but the native TEWL values were restored soon afterward, within 72 hours of incubation. The study showed that an initial interaction between carriers and skin structures occurred to allow the topical delivery of drugs, but without inducing irreversible modifications.
In detail, Figure 2 summarizes the liposomes and liposomal-like vesicles that have been studied to date for the topical treatment of acne and which will be broadly covered in this review. Schematic representation of the advantages of nanomedicine in acne treatment compared to conventional therapies. Liposomes are spherical vesicles, characterized by a phospholipid bilayer and an aqueous core. Although these carriers are not generally able to reach the deeper skin layers, as they are not created as topical drug delivery systems, this allows the delivered drugs to accumulate at the administration site.
In fact, the bilayer can exist in a solid-ordered phase or in a fluid-disordered phase as a function of the employed phospholipids and temperature, as this structural difference could be exploited to trigger the release of the active ingredients.
However, both of the liposomal systems loaded with the antibiotic clindamycin showed improved efficacy in anti-acne clinical studies compared with the free clindamycin lotion. Moreover, no side effects were shown compared to the treatment using the free form of drugs, probably thanks to modulated drug release in terms of time and site. The influence of the surface charge, closely related to the liposomal composition, was also investigated in different studies to clarify its role in topical drug delivery.
This is the case for retinoic acid-loaded positively charged liposomes. Shah et al demonstrated that their positively charged liposomes penetrated into excised pig ear skin more than 3. These data disagree with a more common idea that negatively charged vesicles are more able to cross the skin, because the interaction between opposite charges could otherwise limit the permeation.
An ion-exchange interaction between the cationic vesicles and negative charges of the skin and hair follicle is probably established, but more studies need to be performed to clarify how this interaction could promote the penetration of nanosystems or influence the surface accumulation. The importance of the liposome composition in skin delivery has been demonstrated by Rahman et al. A tretinoin-loaded liposomal formulation made up of The cholesterol was able to reduce vesicle sizes in order to control skin permeation and deposition, while dicetylphosphate significantly enhanced drug release.
Moreover, an increased skin tolerability and patient compliance was shown, and this was due to the drug being protected from exposure to the destabilizing oxygen, light and acids. The commercial gel was more effective than the liposomal formulation.
Based on these assumptions and to improve the efficacy of the formulation, the authors prepared a multidrug formulation. Tetracycline HCl and tretinoin were contained in a carbopol-based liposomal gel in order to exploit the comedolytic and bacteriostatic synergistic effect.
The obtained multidrug formulation showed good technological characteristics in terms of acceptable adhesiveness and viscosity, pH, and controlled and biphasic release of the two drugs.
Finally, the antibacterial efficacy of the formulation has been proven against Staphylococcus aureus and Streptococcus epidermidisand the same minimal biofilm eradication concentration was found when compared to the conventional gel containing the two drugs.
However, the liposomal gel formulation containing the two drugs showed lower minimum inhibitory concentration MIC values against Staphylococcus aureus compared to each solution of the single drug. Another combination therapy, associating retinoic acid 0. Focusing on benzoyl peroxide, its encapsulation in a liposomal formulation led to a significant improvement of drug efficacy against Propionibacteria and Micrococcaceae compared to the other pharmacopoeia benzoyl peroxide formulations.
The ability of liposomes to protect their content drug from external agents, such as light and oxygen, has allowed evaluation of the use of essential oils in the treatment of acne, also increasing their solubilization 37 and reducing their irritating effect on the skin.
Many researchers have already demonstrated the ability of essential oils in the treatment of skin diseases. Essential oils such as tea tree oil, cinnamon oil and rosemary essential oil showed activity against Propionibacterium acne and Staphylococcus epidermis.
Tea tree oil was encapsulated into liposomes to enhance the follicular delivery of this antimicrobial agent. Tea benzac o differin oil-loaded liposomes were formulated, and the cyanoacrylate method was used to evaluate the follicular uptake of vesicles, demonstrating a better targeting ability compared to the other analyzed formulations, microemulsion, multiple emulsion and colloidal bed.
Similarly to liposomes, niosomes are characterized by a highly ordered bilayer and an aqueous core, but in this case the bilayer is made up of non-ionic surfactants for example, cetyl alcohol, decyl glucoside, Brij, polysorbates, spans and poloxamers.
The chemical components of vesicles determine their peculiarities. The non-ionic surfactants that represent the building blocks of the structure can act as permeation enhancers, improving the skin delivery of the encapsulated drug. They probably fuse with the skin surface, enhancing the permeation of drugs through the stratum corneum, owing to their ability to temporarily modify the structure of this barrier.
Because of their apparent advantages, especially in terms of carrier non-toxicity, the potential of niosomes in the treatment of skin diseases, such as acne, was investigated. A comparison study between retinoic acid-loaded liposomes and niosomes was performed to investigate the influence of nanovesicle composition on their cutaneous delivery ability. The study by Manconi et al showed that niosomes penetrate the skin more effectively.
They performed permeation studies using newborn pig skin interposed between donor and receptor compartments of Franz diffusion cells, and concluded that topical drug delivery was strongly affected by the vesicle structure, size and charge obtained using stearylamine or dicetylphosphate as a charge inducer and by the thermodynamic activity of the carried drug.
The authors attributed the good skin-penetrative ability of niosomes to their composition, and in particular to the presence of alkyl polyglucosides APGa class of non-ionic surfactants. Moreover, small negatively charged niosomes, saturated with tretinoin, showed a greater cutaneous retention of drug compared to positively charged vesicles, which, in contrast, could permeate more effectively.
In general, we can assume that vesicles are considered deformable when they are able to cross intact the stratum corneum, deforming themselves and carrying active compounds through the skin Figure 3. The innate deformability of certain topical nanosystems is due to the presence of cosurfactant in their structure, as well as benzac vs oxy type of phospholipids saturated or unsaturated or specific solvent, which influence the ability of the carrier to reach the deeper skin layers to obtain dermal or transdermal delivery.
Ultradeformable vesicles could squeeze through the stratum corneum and reach the deeper skin layers, as described by Cevc and Blume.
Note: Data from references. Topical treatment using liposomes or deformable vesicles. Both the carriers are able to deliver hydrophobic and hydrophilic compounds. Confocal laser scanning micrographs of the interaction between ultradeformable vesicles labeled with rhodamine and Colo cells using: A Hoechst filter and B TRITC filter; and C superimposition of figures. Ultradeformable liposomes as multidrug carrier of resveratrol and 5-fluorouracil for their topical delivery.
Int J Pharm. Vasanth et al, inproposed a gel enriched with vitamin C containing adapalene-loaded ultradeformable vesicles to treat acne. The choice of ultradeformable vesicles for adapalene and vitamin C co-delivery was found to be suitable, as the deformability property of ultradeformable vesicles seems to influence the release kinetics.
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