Formulation of Lipid-Based Nanocarriers of Lacidipine for Improvement of Oral Delivery: Box-Behnken Design Optimization, In Vitro, Ex Vivo, and Preclinical Assessment.

The present research work was aimed to develop and optimize the nanostructured lipid carrier (NLCs) of the antihypertensive drug lacidipine (LAC) for the improvement of oral bioavailability and antihypertensive activity. LAC-NLCs were successfully developed by the preemulsion probe sonication technique. The formulations were optimized by Box-Behnken design and assessed for particle size (PS), polydispersity index (PDI), entrapment efficiency (EE), drug loading (DL), drug release, ex vivo permeation, and in vivo study. The optimized LAC-NLCs showed nanometric PS (191.0 ± 5.89 nm), high EE (90% ± 3.69%) and DL (9.26% ± 1.89%), negative zeta potential (-28.9 ± 0.99 mV), and narrow size distribution (PDI of 0.074 ± 0.013) with spherical morphology. The drug release study revealed that a significantly (p < 0.05) higher LAC release (88.49% ± 3.01%) was achieved from the optimized LAC-NLCs compared to LAC-dispersion (34.27% ± 3.01%). Moreover, the optimized LAC-NLCs showed significantly (p < 0.05) higher intestinal permeation (692.04 ± 19.76 µg) than LAC-dispersion (23.83 ± 5.08 µg). After oral administration of a single dose of LAC, the optimized LAC-NLCs exhibited 3.45-fold higher relative oral bioavailability as well as a more prominent antihypertensive effect than LAC-dispersion. This might be due to the high penetration and absorption of the drug. Hence, NLCs might provide an efficient nano delivery for the management of hypertension and promising drug delivery systems for the bioavailability enhancement of LAC.

Periodontitis and Systemic Disorder-An Overview of Relation and Novel Treatment Modalities.

Periodontitis, a major oral disease, affects a vast majority of the population but has been often ignored without realizing its long-fetched effects on overall human health. A realization in recent years of its association with severe diseases such as carditis, low birth weight babies, and preeclampsia has instigated dedicated research in this area. In the arena of periodontal medicines, the studies of past decades suggest a link between human periodontal afflictions and certain systemic disorders such as cardiovascular diseases, diabetes mellitus, respiratory disorders, preterm birth, autoimmune disorders, and cancer. Although, the disease appears as a locoregional infection, the periodontal pathogens, in addition their metabolic products and systemic mediators, receive access to the bloodstream, thereby contributing to the development of systemic disorders. Mechanism-based insights into the disease pathogenesis and association are highly relevant and shall be useful in avoiding any systemic complications. This review presents an update of the mechanisms and relationships between chronic periodontal infection and systemic disorders. Attention is also given to highlighting the incidence in support of this relationship. In addition, an attempt is made to propose the various periodonto-therapeutic tools to apprise the readers about the availability of appropriate treatment for the disease at the earliest stage without allowing it to progress and cause systemic adverse effects.

Novel nanoemulsion gel containing triple natural bio-actives combination of curcumin, thymoquinone, and resveratrol improves psoriasis therapy: in vitro and in vivo studies.

Curcumin, resveratrol, and thymoquinone are the potential natural bio-actives reported with good anti-psoriatic activity. However, poor aqueous solubility and limited skin permeation of these natural bio-actives hinder their effective delivery and potential therapeutic outcome. In this regard, current research work focuses on the design and optimization of nanoemulsion (NE) gel formulation for the concurrent delivery of these three drugs. The NE system is consisting of oleic acid as oil phase, Tween 20 as surfactant, and PEG 200 as co-surfactant. The optimized formulation exhibited the droplet size 76.20 ± 1.67 nm, PDI of 0.12 ± 0.05, RI of 1.403 ± 0.007, and viscosity of 137.9 ± 4.07 mp. Carbopol 940 (0.5% w/v) was used as the gelling agent to prepare the NE gel which exhibited a good texture profile. The optimized formulation exhibited a higher % of growth inhibition on A-431 cells and demonstrated good anti-angiogenic activity in the HET-CAM test. Finally, in vivo studies in Balb/c mice model showed improved anti-psoriatic conditions which indicated that the triple natural bio-actives combination in nanoemulgel formulation is effective in the management of psoriasis.