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Abstract Background Curcumin (CUR) is a natural polyphenol and one of the key phytoconstituents found in the rhizomes of Curcuma Longa. It exhibits various pharmacological properties, encompassing antioxidant, anticancer effects, antiseptic, and anti-inflammatory, among several others. A significant drawback of using CUR is its limited bioavailability, which primarily depends on gut microorganisms responsible for converting it into its bioavailable form. Therefore, the contemporary study intended to formulate a novel PLAROsomal vesicular delivery of CUR, i.e., CUR-PLAROsomes employing a design of experiments approach to examine the influence of various process parameters, such as particle size and drug percentage release. Result The prepared CUR-PLAROsomes were characterized for their physicochemical properties using various hyphenated tools. The CUR-PLAROsomes exhibited sizes ranging from 40 to 300 nm, and the optimized batch demonstrated a drug entrapment of 86.38 ± 0.22%. In-vitro anticancer studies were conducted using human colorectal adenocarcinoma cells (COLO320DM) and human breast adenocarcinoma (MCF-7). CUR-PLAROsomes exhibited significant in-vivo anti-inflammatory potential against carrageenan-induced paw edema. CUR-PLAROsomes were more potent against COLO320DM and MCF-7 cell lines, even at lower concentrations, than pure CUR. Conclusion Furthermore, based on the observations, it exhibits potential as an anti-inflammatory agent, suggesting that PLAROsomes are an effective vesicular drug delivery system. Highlights Newly introduced PLARosome is a next generation of Liposomes which have gain popularity owing to its better adaptability to overcome leakage problem of vesicular drug delivery system. This is the pioneer attempt to prepare Curcumin-loaded PLARosome as an anti-cancer and anti-inflammatory activity. Nano size of the PLAROsomes may contribute to enhance the efficacy of Curcumin as a target specific drug delivery system. Site specific delivery of phytoconstituents is possible by use of PLAROsomes as a novel drug delivery system. Graphical abstract

Recently, lipid-based nanocarriers have drawn attention as a drug delivery system for numerous illnesses. One novel lipid-based technique is nanocochleate, which is very useful for encapsulating or entrapping the hydrophobic and hydrophilic biological molecules of great importance. This technique helps to protect the entrapped materials from adverse conditions. They have a cylindrical (cigar-like) microstructure in which desired drug substances are trapped, consisting of a lipid bilayer series. Nanocochleates are primarily made up of negatively charged lipids and a divalent cation. They can be formulated using various techniques to ensure the delivery of different active constituents for multiple applications. In addition, nanocochleates enhance the bioavailability of drugs with poor water solubility. Nanocochleates have overcome many disadvantages of other drug delivery systems and have few drawbacks. Because of their exclusive properties and structure, they are the best candidates for oral and systemic drug administration, making them ideal for pharmaceutical preparations. Drug delivery using nanocochleates has previously been used for fungal infections, vaccines, and genes. Recently, nanocochleates have been used to treat several serious, life-threatening illnesses for which conventional therapy falls short. When it comes to drug delivery, nanocochleates may be a better option than other lipid-based methods. This review highlights the fundamentals of nanocochleates, their current status, emerging trends, and potential future applications, underscoring their significance in advancing drug delivery technology and overcoming existing challenges while exploring novel therapeutic avenues.

Studies have reported the potential role of Boswellic acids (BAs), bioactive pentacyclic triterpenes from Boswellia serrata (BS), in treating rheumatoid arthritis (RA). However, poor water solubility and limited oral absorption are restricting factors for its better therapeutic efficacy. Based on these assumptions, the current study aimed to develop naturosomal delivery of BAs to boost their extremely low bioavailability, colloidal stability, and water solubility. Nanonized naturosomes were developed and subsequently analyzed to show their physicochemical and functional features employing the quality-by-design approach. The solubility analysis of Boswellic acid naturosomes revealed a 16 times improvement in aqueous solubility compared to BS extract (BSE). The zeta potential and dynamic light scattering findings of BSE naturosomes (BSENs) have demonstrated their colloidal stability with regulated nano-size particles. Additionally, compared to BSE (⁓31%), in-vitro dissolution experiments showed that >99% of pentacyclic triterpenes were released from BSENs. Studies on ex-vivo permeation showed that BSENs' permeation (>79%) significantly improved over BSE's (⁓20%). In-vivo efficacy studies using CFA-prompted arthritis in rodents showed a critical expansion in body wt and an undeniable reduction in paw thickness, paw volume, and TNF-α treated with BSEN compared to the arthritis control and BSE-treated group. These findings suggest that BSENs can help treat RA drugs by demonstrating their efficacy in further clinical research to validate the significant improvements.

Purpose. The present study aimed to improve the aqueous solubility, permeability, bioavailability, and nootropic potential of standardized Emblica officinalis extract (EOE) by developing a novel phytosomal formulation. Method. Emblica officinalis extract-loaded phytosomes (EOPs) were prepared using solvent evaporation. The EOP was prepared at different molar ratios of extract and phospholipid. Herein, the effects of phospholipid extract ratio (A), temperature (B), and reaction time (C) were systematically investigated on entrapment efficiency using Box-Behnken design. In vitro and in vivo characterizations of the optimized formulation were performed. Results. Optimized EOP formulation (89.90 ± 0.24 μg/ml) exhibited improved aqueous solubility than plain EOE (11.85 ± 0.25 μg/ml). The optimized formulation’s particle size and Zeta potential were 198.4 ± 0.20 nm and −39.0 ± 0.40 mv. DSC and XRD studies confirmed the partial amorphization of EOE in phytosomes. Optimized formulation exhibited 69.82 ± 0.17% of EOE release at 12 h and followed zero-order release kinetics. Moreover, the phytosomal formulation of EOE exhibited its rationality with an improvement of bioavailability by 2.7 folds compared with pure EOE. Compared to EOE, EOP showed significantly (p

Biogenic and biomimetic nanosystems (BBS) are the advanced hybrid nanomaterial used for treatment and diagnosis. These nanosystems' true bench-to-bedside potential makes them a more promising approach for biomedical applications. These nanoparticles are synthesized using biological microorganisms such as bacteria, algae, fungi, etc. A biosynthetic process like extracellular and intracellular biosynthesis can quickly fabricate these nanoparticles. Extracellularly it can be produced from microorganisms and could be between 14 and 16 ​nm. The extracellular enzymes are involved in the biosynthesis of biogenic and biomimetic nanosystems. Moreover, this has proven antifungal and antibacterial activities. Intracellularly, ions can conduct biosynthesis by ions, and crystalline nanosystems can be produced. The present review discusses the various biosynthetic procedures for synthesizing organic and inorganic hybrid nanosystems; additionally, the functionalization of nanosystems is also reported. An external magnetic field is also discussed to target the drug encapsulated in the magnetic nanosystem. The properties of the BBS required for getting the desired outcome in terms of their efficiency and targeted delivery of drugs and the diagnostic property are also given. This review also reports the biomedical applications of these hybrid nanosystems.

The promising therapeutic implications of nanoparticles have spurred their development for biomedical applications. An eco-friendly methodology synthesizes gold nanoparticles using Cordyceps militaris, an edible mushroom (Cord-Au-NPs), using a quality-by-design approach (central composite design). UV-visible spectroscopy analysis revealed an absorption peak at 540–550 nm, thus confirming the synthesis of gold nanoparticles. Cord-Au-NPs have a crystalline structure, as evidenced by the diffraction peaks. The zeta potential value of −19.42 mV signifies the stability of Cord-Au-NPs. XRD study shows gold facets and EDX analysis revealed a strong peak of spherical nanoparticles in the gold region with a mean particle size of 7.18 nm and a polydispersity index of 0.096. The obtained peaks are closely associated with phenolic groups, lipids, and proteins, as examined by FTIR, suggesting that they function as the reducing agent. Cord-Au-NPs exhibited dose-dependent antioxidant, antidiabetic, and antibacterial activity. The method is eco-friendly, nontoxic, less time-consuming, and does not use synthetic materials, leading to higher capabilities in biomedical applications.

Hesperetin (HT) is a polyphenolic compound with anti-carcinogenic, tumor necrosis, and anti-oxidant properties. The present study reports the fabrication, optimization, and evaluation of HT-loaded nanosponges (HTN)- based gel (HTNG) for sustained anti-inflammatory effect. HTN formulation was prepared by quasi emulsion solvent diffusion method using a 42 factorial design. HTN was subjected to different solid and liquid state characterizations and subsequently loaded in carbopol gel. The effects of pro-inflammatory cytokines (IL- 1β and IL-6) were evaluated using RAW 264.7 macrophage cells, and the anti-inflammatory potential was tested in rats. Tiny, porous, and spherical HTN retarded the drug release (39.98%) up to 8 h compared to the pure drug (70.74%) and physical mixture (73.72%) and followed the Higuchi-matrix model. HTNG had a strong downregulating effect on cytokines. It showed no skin irritation and 18.52% skin permeation at 8 h. Further, HTNG-treated rats exhibited 33.16% inflammation inhibition compared to the control group. In conclusion, nanosponges significantly retarded the topical delivery and could circumvent the bioavailability issues associated with HT.

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A reliable RP-HPLC analytical method with UV detection at 421 nm was developed and validated for the quantitative determination of curcumin from rat plasma after oral administration of curcumin loaded nanocochleates (CU-NC) to rats. The chromatographic separation was performed on HIQ SIL, C18 (250 mm × 4.6 mm) column using methanol and water (80:20 v/v) as mobile phase, at 1.0 mL/min flow rate. Validation parameters included linearity, accuracy, precision, and limit of quantitation and detection. Good linearity was obtained over the range of 2.5–100 µg/mL (R2 = 0.9979) of curcumin. The developed HPLC method was precise, with

Role of excipients in designing diverse dosage forms has been highly acclaimed and needs no introduction. These are integral components of pharmaceutical formulations and determine the structure of a dosage form and its function in drug delivery. In many instances, combating the numerous diseases using active therapeutic agents is ultimately challenging task owing to marred solubility and permeability, multidrug resistance, poor pharmacokinetics and associated toxicities, and stability of the drug itself or delivery system. In that context, excipients modulate product aspects such as stability, biopharmaceutical profile, and patient compatibility. D-ɑ-tocopheryl polyethylene glycol succinate (TPGS) is a FDA approved safe and biocompatible adjuvant and acknowledged in pharmaceutical industries for their notable properties namely solubilizer, absorption and permeation enhancer, emulsifier and stabilizer, etc. Moreover, it performs ample bio-functions like anticancer agent, P-gp and cytochrome P450 inhibitor that eventually assist in escalating the therapeutic performance of the drugs. Furthermore, use of TPGS in nanomedicines is reported to be fruitful in improving anticancer potential and pharmacokinetic properties of relevant molecules. By 2025, the international nanomedicine market is projected to reach USD 350.8 billion. Hence, the TPGS-based nanomedicines can emerge as a promising approach for different diseases and can occupy the market in few years. The present review is focused on the pharmaceutical properties of TPGS with the major emphasis on TPGS-based nanomedicines and drug delivery via different routes. Furthermore, the biological and biomedical properties of TPGS are briefed. Thus, use of TPGS in the development of pharmaceutical formulation can be propitious and thus anticipated to offer better therapeutic performance of the cargo.

The present study intends to formulate, characterize and appraise the phospholipid-based nanovesicular system for enhanced delivery of Hesperetin (HT). The quality by design (QbD) approach was employed to prepare Hesperetin naturosomes (HTN) using the solvent evaporation technique and assessed for physicochemical and pharmacological attributes. The FTIR, DSC, and PXRD studies confirmed the successful formation of a vesicular drug-phospholipid complex, while photomicroscopy, SEM, and TEM analysis revealed the morphology of HTN. The functional attributes substantially enhanced the HT's aqueous solubility, drug release, and membrane permeation. The aqueous solubility of HTN was ~10-fold more than that of pure HT. Likewise, the in-vitro dissolution data of HTN showed better competence in releasing the HT (>93%) than the pure HT (~64%) or the physical mixture (~74%). Furthermore, HTN significantly altered HT permeation (>53%) when compared to pure HT (23%) or the physical mixture (28%). The current study showed that naturosomes are a promising way to improve the solubility in water, bioavailability, and therapeutic effectiveness of drugs.