Methods to improve the solubility of therapeutical natural products: a review

Technologies for Solubility, Dissolution and Permeation Enhancement of Natural Compounds

“…Before discussing the modern techniques for the isolation of natural compounds, it should be understood that in modern research, the protocols are carried out as reported by Sarker et al (2005) and given in a Scheme 1 [14]. The modern technique regarding isolation of natural compounds may include; (a) In vitro bioassay-based characterization for the confirmation or final identification of the natural compounds after the achievement of small scale and large scale processing/evaluation parameters as illustrated in Scheme 1, (b) Achievement of such type of compounds in which further modification does not take place from the suitable evaluation parameters and comprehensive review of available literature, (c) Achievement of active moieties with medicinal effectiveness through advanced cell, tissue, genes or vector-based cultures either alone and/or via combinatorial strategy of these, (d) Achievement of sufficient data regarding the efficacy and toxicity profiling of natural compounds, (e) detection of their activity prior to the human-based clinical trials through various in vitro and in silico modeling approaches followed by ex vivo detection and subsequent in vivo animal-based clinical trials, (f) Combining the knowledge regarding selection of only those plant or plant parts which were known for their specific medicinal features (as mentioned earlier) and the modern techniques to achieve the best effective results, and (g) selection of other organisms or part of organism for the evaluation parameters such as marine algae, various bacteria and viruses, even in the modern scientific research cells, antigens or genes could be employed [8][9][10][11][12]. In addition, before initiation of isolation some of the features of natural compounds should be considered including water solubility, pH, size, charge and different types of stability profiles.…”

“…Likewise, a concise insight of natural compounds associated with their enhanced multiple therapeutic effects for cosmetics use and various other biomedical applications has also been portrayed in this review. In contrast, the major dispute associated with natural compounds which could be used on the basis of their therapeutic value is the poor dissolution/solubility and permeation of hydrophobic compounds and various strategies have been investigated to overcome these disputes [7,8].…”

Mimicking Biological Recognition: Lessons in Binding Hydrophilic Guests in Water

“…In this Review, we will focus exclusively on systems that use water‐soluble hosts to bind biological hydrophilic small molecules through non‐covalent interactions. For related topics not covered here, such as supramolecular polymers, [3] anionic recognition, [4, 5] recognition via metal coordination, [5–10] supramolecular drug delivery, [11–13] wider applications of supramolecular chemistry, [14] and more, [15–17] please see the noted reviews.…”

Recent strategies in nanodelivery systems for natural products: a review

“…These unfavourable biopharmaceutical properties often cause low aqueous solubility, poor permeation and absorption through biological membranes and barriers, low biodistribution or rapid metabolism and clearance, resulting in drug plasma levels below the therapeutic concentration and reduced or annulled efficacy. A low bioavailability can be also related to distribution/accumulation of drugs in nontargeted tissues and organs, leading to numerous side effects (Kesarwani et al 2013;Jain & Chella 2020).…”

“…Diverse strategies have been used to optimise the bioavailability of natural products (Dragicevic & Maibach 2016;Jain & Chella 2020;Paroha et al 2020;Saka et al 2020). They are mainly chemical strategies producing semisynthetic compounds or synthetic analogues (Fang & Leu 2006;Ita 2016), but recently there is an increasing interest in developing appropriate formulations, specifically nanodelivery systems, which present numerous advantages in comparison to conventional drug formulations, such as controlled release kinetics, targeted delivery, enhanced solubility and permeation, increased chemical and physical stability, and…”