High-Payload Nanosuspension of Centella asiatica Extract for Improved Skin Delivery with No Irritation

Kim, Eun A; Park, Jun Soo; Kim, Min-Seop; Jeong, Min Ho; Park, Hyun Jin; Choi, Jun Hyuk; Seo, Jin Keun; Choi, Yong Seok; Kang, Myung Joo

doi:10.2147/ijn.s335039

Cited by 16 publications

(3 citation statements)

References 67 publications

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“…However, constraints in the use of C. asiatica extracts for wound healing are the low solubility in water because of the high molecular weight of the active ingredients. The solubility of ingredients affects wound healing, and insolubility or very poor solubility in water [ 22 ] negatively affects absolute bioavailability [ 23 ]. Therefore, we aimed to use carboxymethyl-cellulose (CMC) as a solvent for the crude extract of C. asiatica , because it is a good solvent for the target active ingredients in wound healing [ 24 ].…”

Section: Introductionmentioning

confidence: 99%

RETRACTED: Centella asiatica extract in carboxymethyl cellulose at its optimal concentration improved wound healing in mice models

Tanga¹,

Bang²,

Fang³

et al. 2022

Heliyon

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Section: Introductionmentioning

confidence: 99%

RETRACTED: Centella asiatica extract in carboxymethyl cellulose at its optimal concentration improved wound healing in mice models

Tanga¹,

Bang²,

Fang³

et al. 2022

Heliyon

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“…Mechanical grinding using media milling beads has the following advantages: low energy utilization, ease of scale-up, no organic solvent use, and minimum batch-to-batch variation compared to other nanosizing techniques. [49][50][51][52] Dual centrifugation, a wet ball milling lab-scale type, pulverizes the raw material by additional sample rotation during the centrifugal process with zirconia beads, resulting in vigorous movement of the samples inside the vials with beads. This eventually results in their rapid homogenization or milling.…”

Section: Screening Of Suspending Agent Of Mtk Crystalline Suspensionmentioning

confidence: 99%

Design of Montelukast Nanocrystalline Suspension for Parenteral Prolonged Delivery

Park¹,

Kim²,

Joung³

et al. 2022

IJN

Self Cite

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Background: Montelukast (MTK), a representative leukotriene receptor antagonist, is currently being investigated as a potential candidate for treating Alzheimer's disease. For potent and effective dosing in elderly patients, a parenteral prolonged delivery system is favored, with improved medication adherence with reduced dosage frequency. Purpose: This study aimed to design a nanocrystalline suspension (NS)-based MTK prolonged delivery system and evaluate its pharmacokinetics profile and local tolerability following subcutaneous administration. Methods: To decelerate the dissolution rate, the amorphous MTK raw material was transformed into a crystalline state using a solvent-mediated transformation method and subsequently formulated into NS using a bead-milling technique. The MTK NSs were characterized by morphology, particle size, crystallinity, and in vitro dissolution profiles. The pharmacokinetic profile and local tolerability at the injection site following subcutaneous injection of MTK suspension were evaluated in rats. Results: Microscopic and physical characterization revealed that the amorphous MTK powder was lucratively transformed into a crystalline form in acidic media (pH 4). MTK crystalline suspensions with different diameters (200 nm, 500 nm, and 3 μm) were uniformly prepared using bead-milling technology, employing polysorbate 80 as suspending agent. Prepared crystalline suspensions exhibited analogous crystallinity (melting point, 150°C) and size-dependent in vitro dissolution profiles. MTK NSs with particle sizes of 200 nm and 500 nm provided a protracted pharmacokinetic profile for up to 4 weeks in rats, with a higher maximum drug concentration in plasma than the 3 μm-sized injectable suspensions. Histopathological examination revealed that MTK NS caused chronic granulomatous inflammation at the injection site, which resolved after 4 weeks. Conclusion:The MTK parenteral NS delivery system is expected to be a valuable tool for treating Alzheimer's disease with extended dose intervals.

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“…Hence, to address these limitations, polymeric nanocarriers are needed to sustain the release of MAD for an extended period. 1 Kim et al prepared Centella asiatica-loaded nanocrystal suspensions and reported the drug release for 4 h. 2 Similarly, Yongsirasawad and co-workers developed Centella asiatica extract-loaded gelatin nanoparticles using one-step desolvation method and demonstrated drug release for almost 3.5 h. 3 Still, much work needs to be done. Therefore, to overcome the limitations of MAD, the authors made an effort to develop polymeric nanogels of chitosan for sustained delivery of MAD.…”

Section: Introductionmentioning

confidence: 99%

Formulation and In Vitro Assessment of Polymeric pH-Responsive Nanogels of Chitosan for Sustained Delivery of Madecassoside

Suhail,

Chiu,

Ullah

et al. 2024

ACS Omega

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Madecassoside, a triterpenoid saponin compound mainly isolated from the gotu kola herb (Centella asiatica), shows an extensive range of biological activities, including antiapoptotic, antioxidant, anti-inflammatory, moisturizing, neuroprotective, and wound healing effects. It has been highly used in the management of eczema, skin wounds, and other diseases. Due to poor oral bioavailability, membrane permeability, and intestinal absorption, the clinical application of the madecassoside is limited. Hence, a drug carrier system is needed that not only sustains the release of the madecassoside but also overcomes the drawbacks associated with its administration. Therefore, the authors prepared novel pH-responsive chitosan-based nanogels for the sustained release of madecassoside. Free radical polymerization technique was used for cross-linking of polymer chitosan and monomer methacrylic acid in the presence of cross-linker N′,N′-methylene bis(acrylamide). The decrease in polymer crystallinity after polymerization and development of nanogels was demonstrated by XRD and FTIR analysis. The effects of nanogel contents on polymer volume, sol–gel analysis, swelling, drug loading, and release were investigated. Results indicated that high swelling and maximum release of the drug occurred at pH 7.4 compared to pH 1.2 and 4.6, indicating the excellent pH-sensitive nature of the engineered nanogels. High swelling and drug release were perceived with the integration of a high quantity of chitosan, while a decline was observed with the high integration of N′,N′-methylene bis(acrylamide) and methacrylic acid contents. The same effects of nanogel contents were shown for drug loading too. Sol fraction was reduced, while gel fraction was enhanced by increasing the chitosan load, N′,N′-methylene bis(acrylamide), and methacrylic acid. The Korsmeyer–Peppas model of kinetics was trailed by all nanogel formulations with non-Fickian diffusion. The results demonstrated that prepared nanogels can be employed for sustained release of the madecassoside.

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High-Payload Nanosuspension of Centella asiatica Extract for Improved Skin Delivery with No Irritation

Cited by 16 publications

References 67 publications

RETRACTED: Centella asiatica extract in carboxymethyl cellulose at its optimal concentration improved wound healing in mice models

RETRACTED: Centella asiatica extract in carboxymethyl cellulose at its optimal concentration improved wound healing in mice models

Design of Montelukast Nanocrystalline Suspension for Parenteral Prolonged Delivery

Formulation and In Vitro Assessment of Polymeric pH-Responsive Nanogels of Chitosan for Sustained Delivery of Madecassoside

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