Co-crystallization is a promising approach for improving physical and pharmacological properties of API, viz., solubility, dissolution rate, stability, hygroscopicity, tablet ability, mechanical properties, bioavailability, and therapeutic efficacy. Different methods for the preparation of pharmaceutical co-crystals have been discussed. Instrumental and physicochemical characterization methods have also been included. Herbal bioactives are potential candidates for co-crystallization to improve solubility, mask taste, and improve bioavailability. Literature on the development of co-crystals of herbal bioactives like curcumin, quercetin, berberine, resveratrol, naringenin, and miscellaneous herbal compounds has been reported systematically in the present review. In conclusion, co-crystallization of herbal bioactives is a promising method for enhancing their physical properties. However, toxicological, stability, regulatory, and scaleup issues must be adequately addressed before commercial viability can be expected.

The rectal route is an effective route for the local and systemic delivery of active pharmaceutical ingredients. The environment of the rectum is relatively constant with low enzymatic activity and is favorable for drugs having poor oral absorption, extensive first-pass metabolism, gastric irritation, stability issues in the gastric environment, localized activity, and for drugs that cannot be administered by other routes. The present review addresses the rectal physiology, rectal diseases, and pharmaceutical factors influencing rectal delivery of drugs and discusses different rectal drug delivery systems including suppositories, suspensions, microspheres, nanoparticles, liposomes, tablets, and hydrogels. Clinical trials on various rectal drug delivery systems are presented in tabular form. Applications of different novel drug delivery carriers viz. nanoparticles, liposomes, solid lipid nanoparticles, microspheres, transferosomes, nano-niosomes, and nanomicelles have been discussed and demonstrated for their potential use in rectal administration. Various opportunities and challenges for rectal delivery including recent advancements and patented formulations for rectal drug delivery have also been included.

Co-processing involves the incorporation of one excipients into the particle structure of other excipients to overcome the deficiencies of each excipients. The current patent describes the co-processing of microcrystalline cellulose and mannitol via fluid bed agglomeration with an aim to limit the use of lubricant in tablet composition. The co-processed excipients blend was compared with the physical blend of excipients and characterized for scanning electron microscopy, disintegration and hardness. The average particle size of co-processed excipients was less than 0.55 mm, characterized by large individual lactose coated particles whereas, the physical blend particles are uncoated and irregular in shape. Tablets made from both physical blend and co-processed excipients were compared. As per the hardness and disintegration studies, with increase in mixing time of excipients both hardness and disintegration time decreases.

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Co-crystallization is a technique for modifying physicochemical properties of pharmaceutical ingredients with an aim to enhance the therapeutic efficacy and subsequent reduction in toxicity. The patent describes the development of oxaliplatin co-crystals using flavonoids (baicalein and naringenin) via solvent volatilization technique with an objective to improve solubility and stability in GI tract and reduced side/toxic effects. The co-crystals were characterized via differential scanning calorimetry, thermogravimetric analysis, x-ray diffraction analysis. The co-crystals exhibited slow drug release, delayed hydrolysis, low cytotoxicity and enhanced therapeutic activity on human gastric adenocarcinoma cells. However, suitable solvent for co-crystal production, large scale production and regulatory challenges for continuous manufacturing of co-crystals must be addressed.