Nanotechnological Advances for Cutaneous Release of Tretinoin: An Approach to Minimize Side Effects and Improve Therapeutic Efficacy

Raminelli, Ana Claudia Pompeu; Romero, Valéria; Semreen, Mohammad H.; Leonardi, Gislaine Ricci

doi:10.2174/0929867325666180313110917

Cited by 22 publications

(11 citation statements)

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“…A total of 2 mL of the sample was withdrawn from the receptor compartment at definite time intervals and replaced with an equal volume of fresh receptor fluid. The aliquots were suitably diluted with the receptor medium and analysed by HPLC method 14 – 16 . In vitro drug release kinetics To investigate the release mechanism of CLN-free base from the microsponge loaded gels, the release data was analysed using zero order, first order, Higuchi, Hixson-Crowell, and Korsmeyer-Peppas.…”

Section: Methodsmentioning

confidence: 99%

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Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

Khattab

Nattouf

2021

Sci Rep

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The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

Khattab

Nattouf

2021

Sci Rep

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“…Ramenelli et al [66] recently reviewed the nano delivery system approaches that have been applied to tretinoin including liposomes, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, cyclodextrins and nanostructured polymers. Some examples are described below and other studies are summarized in Table 3 [51,52,67,68,69,70,71].…”

Section: Targeted Topical Delivery Of Retinoids: Strategies To Impmentioning

confidence: 99%

Targeted Topical Delivery of Retinoids in the Management of Acne Vulgaris: Current Formulations and Novel Delivery Systems

et al. 2019

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Acne vulgaris is a common inflammatory pilosebaceous condition that affects 80–90% of adolescents. Since the introduction of tretinoin over 40 years ago, topical retinoid products have been a mainstay of acne treatment. The retinoids are very effective in addressing multiple aspects of the acne pathology as they are comedolytic and anti-inflammatory, and do not contribute to antibiotic resistance or microbiome disturbance that can be associated with long-term antibiotic therapies that are a common alternative treatment. However, topical retinoids are associated with skin dryness, erythema and pain, and may exacerbate dermatitis or eczema. Thus, there is a clear need to target delivery of the retinoids to the pilosebaceous units to increase efficacy and minimise side effects in surrounding skin tissue. This paper reviews the current marketed topical retinoid products and the research that has been applied to the development of targeted topical delivery systems of retinoids for acne.

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“…All‐ trans ‐retinoic acid (RA), also known as tretinoin or retinoic acid, is the acidic form of vitamin A and have been widely used for topical application in the treatment of acne, wrinkles, hyperpigmentation, keratinization disorders, stretch marks, and cellulitis 1,2 . Nevertheless, despite its effects on skin treatment, the application of this drug is limited due to its chemical instability in the presence of light and oxygen and poor aqueous solubility 2,3 . In addition, RA treatment can result in a high incidence of side effects, including erythema, irritation, burning, scaling, and dermatitis, which negatively affects patient compliance 1,4,5 …”

Section: Introductionmentioning

confidence: 99%

“…Many strategies have been studied to ensure efficient application and to reduce the unwanted characteristics of RA, such as the encapsulation methodology using controlled delivery systems. Besides protecting RA, these systems can reduce the side effects and improve the permeation profile to potentiate efficacy and safety on the skin 2 . A variety of innovative delivery vehicles have been developed to encapsulate RA, including liposomes, nanocapsules, and solid lipid particles 6–9 .…”

Section: Introductionmentioning

confidence: 99%

Biopolymer‐based microparticles for encapsulation of all‐trans‐retinoic acid

Silva

Dambros

Leonardi

et al. 2021

J of Applied Polymer Sci

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This work aims to investigate the potential of complex coacervation technique to encapsulate and protect all‐trans retinoic acid (RA). Gelatin and κ‐carrageenan were used as wall material and pequi oil was employed as a hydrophobic phase. Three formulations with different protein: polysaccharide ratio and pH were defined to produce the microparticles based on the zeta potential and turbidity analysis: (F1) ratio 3:1 and pH 3.5, (F2) ratio 8:1 and pH 3.5, and (F3) ratio 8:1 and pH 5.0. Microparticles were evaluated regarding their morphology, yield, encapsulation efficiency (EE), and stability. The properties of microparticles were mainly affected by the protein: polysaccharide ratio and the turbidity of the mixtures, which is directly related to the protein‐polysaccharide interaction. Formulation 1 showed the optimal values of yield (75.6%), EE (100.2%), and stability (85% of the encapsulated RA remained in the particle). The results demonstrated the high potential of this innovative technique to encapsulate RA for a future application in topical formulations.

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Nanotechnological Advances for Cutaneous Release of Tretinoin: An Approach to Minimize Side Effects and Improve Therapeutic Efficacy

Abstract: As evident from the literature, the tretinoin technological delivery systems consist an innovative and potential management for increasing the patient compliance presenting safety and efficacy.

Cited by 22 publications

References 0 publications

Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

Targeted Topical Delivery of Retinoids in the Management of Acne Vulgaris: Current Formulations and Novel Delivery Systems

Biopolymer‐based microparticles for encapsulation of all‐trans‐retinoic acid

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