“…While a reduced concentration of liquid lipid in BM leads to the formulation of an imperfect type of NLCs, a high percentage of oil can form separate oil nanoparticles, which may lead to phase separation during or after the formulation preparation. 15 Additionally, a complementary filter paper method was used to visually assess any presence of oil droplets in the BM as an indication of phase separation. 34 The results demonstrated that no oil droplets on the filter paper were visually observed when the OA concentration was used up to 30% in BM.…”
Section: Resultsmentioning
confidence: 99%
“…Polysorbate 80 as a non-ionic surfactant has been used extensively in the preparation of topical formulations with minimal issues of irritation reported, while it can also help to increase membrane permeability to poorly soluble drugs by altering membrane fluidity. 15 , 45 Similarly, Stearoyl polyoxyl-32 glycerides is a non-ionic poly ethylene glycol ester surfactant with an excellent emulsification capacity, which has also been used to prepare various NLCs. 46 Figure 3 Particle size and polydispersity index of the preliminary nanostructured lipid carriers prepared from various surfactants and surfactant mixtures.…”
Section: Resultsmentioning
confidence: 99%
“…The purge gas (nitrogen) was applied at a flow rate of 50 mL/min. The width of melting events and crystallinity index were obtained by substituting in the following equations: 15 International Journal of Nanomedicine 2023:18 https://doi.org/10.2147/IJN.S400610…”
Section: Determination Of the Binary Mixture Ratiomentioning
confidence: 99%
“…On the other hand, matrix-type patches containing NLCs have been considered as an alternative dosage form for topical application as they can offer several clinical advantages where they can be cut to any size while significantly reducing dosing frequencies and providing good protection of the formulation from the external environment. 15 , 16 …”
Section: Introductionmentioning
confidence: 99%
“…On the other hand, matrix-type patches containing NLCs have been considered as an alternative dosage form for topical application as they can offer several clinical advantages where they can be cut to any size while significantly reducing dosing frequencies and providing good protection of the formulation from the external environment. 15,16 Preparation of NLCs involves many experimental components, each with a potentially significant contribution to the quality of the final product. The design of experiments (DoE) has gained significant attention as a systematic approach to understanding the technical process and variables that can significantly affect the output of a pharmaceutical product.…”
Background
Imiquimod (IMQ) is an immunomodulating drug that is approved for the treatment of superficial basal cell carcinoma, actinic keratosis, external genital warts and perianal warts. However, IMQ cream (Aldara
®
) has several drawbacks including poor skin permeation, local toxicity, and compromised patient compliance as a topical pharmacological option.
Methods
Our research aimed to develop and optimize nanostructured lipid carriers (NLCs) containing IMQ for the first time using a hybrid design of experiments approach. The optimized formulation was then incorporated into a matrix-type topical patch as an alternative dosage form for topical application and evaluated for IMQ deposition across different skin layers in comparison to the performance of the commercial product. Additionally, our work also attempted to highlight the possibility of implementing environment-friendly practices in our IMQ-NLCs formulation development by reviewing our analytical methods and experimental designs and reducing energy and solvent consumption where possible.
Results
In this study, stearyl alcohol, oleic acid, Tween
®
80 (polysorbate 80), and Gelucire
®
50/13 (Stearoyl polyoxyl-32 glycerides) were selected for formulation development. The formulation was optimized using a 2
k
factorial design and a central composite design. The optimized formulation achieved the average particle size, polydispersity index, and zeta potential of 75.6 nm, 0.235, and – 30.9 mV, respectively. Subsequently, a matrix-type patch containing IMQ-NLCs was developed and achieved a statistically significant improvement in IMQ deposition in the deeper skin layers. The IMQ deposition from the patch into the dermis layer and receptor chamber was 3.3 ± 0.9 µg/cm
2
and 12.3 ± 2.2 µg/cm
2
, while the commercial cream only deposited 1.0 ± 0.8 µg/cm
2
and 1.5 ± 0.5 µg/cm
2
of IMQ, respectively.
Conclusion
In summary, IMQ-NLC-loaded patches represent great potential as a topical treatment option for skin cancer with improved patient compliance.
“…While a reduced concentration of liquid lipid in BM leads to the formulation of an imperfect type of NLCs, a high percentage of oil can form separate oil nanoparticles, which may lead to phase separation during or after the formulation preparation. 15 Additionally, a complementary filter paper method was used to visually assess any presence of oil droplets in the BM as an indication of phase separation. 34 The results demonstrated that no oil droplets on the filter paper were visually observed when the OA concentration was used up to 30% in BM.…”
Section: Resultsmentioning
confidence: 99%
“…Polysorbate 80 as a non-ionic surfactant has been used extensively in the preparation of topical formulations with minimal issues of irritation reported, while it can also help to increase membrane permeability to poorly soluble drugs by altering membrane fluidity. 15 , 45 Similarly, Stearoyl polyoxyl-32 glycerides is a non-ionic poly ethylene glycol ester surfactant with an excellent emulsification capacity, which has also been used to prepare various NLCs. 46 Figure 3 Particle size and polydispersity index of the preliminary nanostructured lipid carriers prepared from various surfactants and surfactant mixtures.…”
Section: Resultsmentioning
confidence: 99%
“…The purge gas (nitrogen) was applied at a flow rate of 50 mL/min. The width of melting events and crystallinity index were obtained by substituting in the following equations: 15 International Journal of Nanomedicine 2023:18 https://doi.org/10.2147/IJN.S400610…”
Section: Determination Of the Binary Mixture Ratiomentioning
confidence: 99%
“…On the other hand, matrix-type patches containing NLCs have been considered as an alternative dosage form for topical application as they can offer several clinical advantages where they can be cut to any size while significantly reducing dosing frequencies and providing good protection of the formulation from the external environment. 15 , 16 …”
Section: Introductionmentioning
confidence: 99%
“…On the other hand, matrix-type patches containing NLCs have been considered as an alternative dosage form for topical application as they can offer several clinical advantages where they can be cut to any size while significantly reducing dosing frequencies and providing good protection of the formulation from the external environment. 15,16 Preparation of NLCs involves many experimental components, each with a potentially significant contribution to the quality of the final product. The design of experiments (DoE) has gained significant attention as a systematic approach to understanding the technical process and variables that can significantly affect the output of a pharmaceutical product.…”
Background
Imiquimod (IMQ) is an immunomodulating drug that is approved for the treatment of superficial basal cell carcinoma, actinic keratosis, external genital warts and perianal warts. However, IMQ cream (Aldara
®
) has several drawbacks including poor skin permeation, local toxicity, and compromised patient compliance as a topical pharmacological option.
Methods
Our research aimed to develop and optimize nanostructured lipid carriers (NLCs) containing IMQ for the first time using a hybrid design of experiments approach. The optimized formulation was then incorporated into a matrix-type topical patch as an alternative dosage form for topical application and evaluated for IMQ deposition across different skin layers in comparison to the performance of the commercial product. Additionally, our work also attempted to highlight the possibility of implementing environment-friendly practices in our IMQ-NLCs formulation development by reviewing our analytical methods and experimental designs and reducing energy and solvent consumption where possible.
Results
In this study, stearyl alcohol, oleic acid, Tween
®
80 (polysorbate 80), and Gelucire
®
50/13 (Stearoyl polyoxyl-32 glycerides) were selected for formulation development. The formulation was optimized using a 2
k
factorial design and a central composite design. The optimized formulation achieved the average particle size, polydispersity index, and zeta potential of 75.6 nm, 0.235, and – 30.9 mV, respectively. Subsequently, a matrix-type patch containing IMQ-NLCs was developed and achieved a statistically significant improvement in IMQ deposition in the deeper skin layers. The IMQ deposition from the patch into the dermis layer and receptor chamber was 3.3 ± 0.9 µg/cm
2
and 12.3 ± 2.2 µg/cm
2
, while the commercial cream only deposited 1.0 ± 0.8 µg/cm
2
and 1.5 ± 0.5 µg/cm
2
of IMQ, respectively.
Conclusion
In summary, IMQ-NLC-loaded patches represent great potential as a topical treatment option for skin cancer with improved patient compliance.
Acrylic pressure‐sensitive adhesives (PSAs) were synthesized using a solvent‐free ultraviolet‐induced polymerization method. The monomers n‐(isobutoxymethyl) acrylamide, 2‐ethylhexyl acrylate, 2‐hydroxyethyl acrylate, and methyl methacrylate and an initiator, hydroxy dimethyl acetophenone, were used to prepare acrylic copolymers as prepolymers. A multifunctional monomer, trimethylolpropane triacrylate, was added to form a semi‐interpenetrating network, leading to an increase in the modulus and elasticity of the prepolymer. This decreased the peel strength, which is suitable for temporary protective films. Rheological data from small‐amplitude oscillatory shear measurements also revealed consistent results suitable for removable PSAs. The plasticizers, such as dioctyl phthalate and dioctyl terephthalate, possessing favorable interactions with the main resins were found to exhibit transparency, clear debonding, and ultralow release, which are essential features for temporary protective films.
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