article · Drug Design Development and Therapy
This study focuses on developing elastic nanovesicles, known as nanospanlastics, to improve the topical delivery of 3-acetyl-11-keto-beta-boswellic acid. Although the compound possesses potent anti-inflammatory properties, its high lipophilicity hampers topical administration, and poor aqueous solubility limits oral bioavailability. Formulations were created using an ethanol injection method with Span 60 as a surfactant and Tween 80 as an edge activator, evaluated through a factorial experimental design. The leading formulation, designated F7, achieved an entrapment efficiency of 90.04 percent, released 96.87 percent of the drug over eight hours, and maintained a particle size of 255.8 nanometres. Microscopic and thermal analysis confirmed well-defined spherical vesicles without harmful interactions between the compound and excipients. The formulation remained physically and chemically stable after three months of refrigerated storage, showing significantly enhanced skin permeation in rat skin tests compared to the unformulated drug.
Plant-derived anti-inflammatory compounds often fail to reach their therapeutic potential because the skin acts as a barrier against highly lipophilic molecules. By encapsulating such compounds in flexible nanovesicles, formulation scientists can substantially improve skin penetration. This offers a viable approach to developing topical treatments that deliver effective doses of natural therapeutic agents directly through the skin without relying on oral administration.
This work is early-stage experimental research that could enable topical anti-inflammatory formulations for pharmaceutical and dermatological development. The primary users would be formulation scientists and drug developers looking to deliver lipophilic active ingredients topically. Because testing has only progressed through laboratory characterisation and ex vivo rat skin permeation models, significant further evaluation, including in vivo efficacy and clinical trials, is required before real-world commercial use.
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Purpose: The current study aimed to discuss the potential of nanospanlastics as a surfactant-based vesicular system for improving the topical delivery of 3-acetyl-11-keto-β-boswellic acid (AKBA). AKBA is a potent anti-inflammatory drug, but it has poor oral bioavailability due to its poor aqueous solubility. Moreover, the topical delivery of AKBA is difficult due to its high lipophilicity. To overcome these drawbacks, AKBA was formulated as deformable elastic nanovesicles and nanospanlastics, for improving its topical delivery. Materials and Methods: AKBA-loaded spanlastic nanovesicles (SNVs) were formulated by ethanol injection technique according to 2 3 factorial design using Span 60 as a non-ionic surfactant and Tween 80 as edge activator (EA) to investigate the effect of different independent variables on entrapment efficiency (EE%), % drug released after 8 hr (Q 8h ) and particle size (PS) using Design-Expert software. In vitro characterization, stability test and ex vivo permeation study of the optimized formula were performed. Results: The choice of the optimized formula was based on the desirability criteria. F7 was selected as the optimized formula because it has the highest desirability value of 0.648. F7 exhibited EE% of 90.04± 0.58%, Q 8h of 96.87± 2.67%, PS of 255.8± 2.67 nm, and zeta potential of − 49.56 mV. F7 appeared as spherical well-defined vesicles in both scanning electron microscope (SEM) and transmission electron microscope (TEM). The Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies investigated the absence of interaction between AKBA and different excipients and good encapsulation of AKBA within SNVs. F7 retained both physical and chemical stability after storage for 3 months at 4– 8 °C. Ex vivo permeation test exhibited significant enhancement of permeability of F7 across rat skin than the free drug. Conclusion: Nanospanlastics could be a promising approach for improving the permeability and topical delivery of AKBA. Keywords: AKBA, spanlastics, topical delivery, optimization, edge activator
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DOI: 10.2147/dddt.s265167
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