Recent Patents on Drug Delivery & Formulation

Publisher: Bentham Science Publishers

Journal description

Recent Patents on Drug Delivery & Formulation publishes review articles by experts on recent patents on drug delivery and formulation. A selection of important and recent annotated patents on drug delivery and formulation is also included in the journal. The journal is essential reading for all researchers involved in the fields of drug delivery and formulation.

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Website Recent Patents on Drug Delivery and Formulation website
Other titles Recent patents on drug delivery and formulation, Drug delivery & formulation, Drug delivery and formulation
ISSN 1872-2113
OCLC 163586653
Document type Journal / Magazine / Newspaper

Publisher details

Bentham Science Publishers

  • Pre-print
    • Author can archive a pre-print version
  • Post-print
    • Author cannot archive a post-print version
  • Restrictions
    • 12 months embargo
  • Conditions
    • Author's pre-print on author's personal website, institutional repository and open access repository
    • Author's post-print on author's personal website, institutional repository, open access repository, PubMed Central and arXiv
    • Non-Commercial
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    • Must link to journal home page with DOI
    • Publisher's version/PDF cannot be used
  • Classification
    ​ yellow

Publications in this journal

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    ABSTRACT: Microneedles have been developed in the past few years as a new transdermal drug delivery mean. They indeed present many advantages compared to injections using hypodermic needles (reduced contaminations and epidermic reactions risks), but mostly bring comfort and compliance to patients. Microneedles may be plain and open pathways for medications though the skin, dissolving into it, or hollow and allow fluid to actually enter the dermis or the hypodermis. This review focuses on this last type of microneedles and their problematic in terms of application, which are of two types: first insure correct insertion into the skin (controlled and repeatable insertion depth mainly), second insure correct fluid delivery to the dermis (controlled infusion rate). This paper thus focuses on recently published patents about hollow microneedle applicators, i.e. microneedles applicators that allow fluid delivery to the skin. A description of several most relevant patents concerning the technology is given. The benefits and drawbacks of the different solutions are also described.
    Recent Patents on Drug Delivery & Formulation 03/2015;
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    ABSTRACT: Increased prevalence of oral diseases such as gingivitis, periodontitis and dental caries has become major health issue worldwide. Such growing incidence of periodontitis has directly affected the development of drug delivery systems and growth of the market. Since the infections are limited to periodontal pockets or oral cavity, localized intrapocket drug delivery will be more beneficial than conventional systemic administration. Advances in intrapocket technology and innovations in the field of periodontal drug delivery led to increased patent applications. Newer trends like use of mucoadhesive polymers, in situ forming gels, viscosity modifiers, plasticizers etc which can enhance intrapocket retention of drugs have gained considerable attention among researchers and industrialists. Current market is flooded with products such as Periostat, Periochip®, Atridox®, Arestin®, Actisite®, Dentomycin®, and Elyzol® and generics such as metronidazole, levofloxacin, tetracycline, doxycyline and minocycline for intrapocket delivery. There is a need of novel drugs and delivery systems with better efficacy profiles than the existing compounds. Inclusion of novel technologies like films, fibers, in situ forming implants, microparticles, nanoparticles, and liposomes as intrapocket drug delivery has great potential. Development of antibiotic free drug delivery such as antiseptics, host modulators, biofilms inhibitors and antibodies has promising role in the improvement of pathogenesis of periodontitis. Further, this review deals with various innovations in drug delivery and patents related to localized intrapocket administration of medicaments in the implications of periodontitis.
    Recent Patents on Drug Delivery & Formulation 03/2015; 09(999). DOI:10.2174/1872211309666150311095424
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    ABSTRACT: Objective: Norfloxacin has a low aqueous solubility which leads to poor dissolution. Keeping this fact in mind the purpose of this study is to formulate and evaluate norfloxacin solid dispersion. Methods: Solid dispersions of various ratios were prepared using hydrophilic carriers like polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974pNF (CP). All of these formulations were prepared using solvent evaporation technique. These formulations were evaluated using solubility studies, dissolution studies; Fourier transmitted infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetery (DSC). The influence of polymer type and drug to polymer ratio on the solubility and dissolution rate of norfloxacin was also evaluated. Results: FTIR analysis showed no interaction of all three polymers with norfloxacin. The results from XRD and DSC analyses of the solid dispersion preparations showed that norfloxacin was in its amorphous form. Among the Norfloxacin: PEG solid dispersions, Norfloxacin: PEG 1:14 ratio showed the highest dissolution rate at pH 6.8. For norfloxacin: PVP solid dispersions, norfloxacin: PVP 1:10 ratio showed the highest dissolution rate at pH 6.8. For Norfloxacin: CP solid dispersions, norfloxacin: P 1:2 ratio showed the highest dissolution rate at pH 6.8.Conclusion: The solid dispersion of norfloxacin with polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974p NF (CP), lends an ample credence for better therapeutic efficacy.
    Recent Patents on Drug Delivery & Formulation 02/2015; 09(999). DOI:10.2174/1872211309666150225124424
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    ABSTRACT: By the virtue of their nature, cosmetic products are used to clean, perfume, change the appearance of the human body's various external parts and maintain them in a good condition. Their main sites of action may be exemplified by the nails, the hair system, the epidermis, the external genital organs and the mucous membranes of the oral cavity. Sunscreen preparations consist of organic chemicals and inorganic materials. Inorganic materials include chemicals that scatter UV physically like TiO2 and ZnO. Organic materials such as avobenzone reduce the amount of UV light to which the human skin is exposed by absorbing the radiation and subsequent disposal in different ways. One of the way of disposal may be by undergoing photoinduced decompositions which not only cause a reduction of the sunscreen UV-protective capacity during usage but may precipitate allergic or toxic degradates. Thus undoubtedly a high photostability is an important requirement for the effectiveness of sunscreen products. Many researchers patented their work on this aspect of protection of avobenzone from photodegradation using varying methodology. This review article discusses some of the patented works done in enhancing the photostability of avobenzone and its formulations.
    Recent Patents on Drug Delivery & Formulation 01/2015;
  • Recent Patents on Drug Delivery & Formulation 01/2015;
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    ABSTRACT: Less than 8.5% of ischemic stroke patients receive clot-busting drugs within the narrow time needed to reduce injury. Thus, there is need for an easily-accessible delayed post-stroke drug treatment to improve functional recovery. Various combinations of fluoxetine, simvastatin, and ascorbic acid were given to healthy rats to assess impact on neurogenesis versus controls. Fluoxetine combined with simvastatin and ascorbic acid produced a 19-fold increase in neurogenesis versus controls in healthy rats; fluoxetine alone produced 10-fold increase. We next tried a couple of drug combinations versus control in endothelin-induced stroked rats. Combined fluoxetine/simvastatin/ascorbic acid treatment, given to stroked rats 20-26 hours after stroke induction and continued for 31 days, produced strong recovery as measured by Montoya staircase test (mean recovery to 85% of pre-stroke function) and Forelimb Asymmetry test (mean recovery to 90% of pre-stroke function) . Fluoxetine and ascorbic acid without simvastatin only produced ~50% of recovery produced by the 3-drug combination. Our results indicate that combined treatment of Fluoxetine, simvastatin and ascorbic acid represents a promising delayed stroke treatment that greatly improves functional recovery in rats and warrants further study in human patient populations. This work formed the basis for a patent submission (US20130065924A1) Composition and method for treatment of neurodegeneration.
    Recent Patents on Drug Delivery & Formulation 01/2015;
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    ABSTRACT: Hypothalamic releasing and inhibiting hormones are major neuroendocrine regulators of human body metabolism being driven directly to the anterior pituitary gland via hypothalamic-hypophyseal portal veins. The alternative physiological or therapeutic interventions utilizing the pharmaco-nutritional boost of imidazole-containing dipeptides (non-hydrolized oral form of carnosine, carcinine, N-acetylcarnosine lubricant eye drops) can maintain health, enhance physical exercise performance and prevent ageing. Carnosine (β-alanyl-L-histidine) is synthesized in mammalian skeletal muscle. There is an evidence that the release of carnosine from the skeletal muscle sarcomeres moieties during physical exercise affects autonomic neurotransmission and physiological functions. Carnosine released from skeletal muscle during exercise acts as a powerful afferent physiological signaling stimulus for hypothalamus, may be transported into the hypothalamic tuberomammillary nucleus (TMN), specifically to TMN-histamine neurons and hydrolyzed herewith via activities of carnosine-degrading enzyme (carnosinase 2) localized in situ. Through the colocalized enzymatic activity of Histidine decarboxylase in the histaminergic neurons, the resulting L-histidine may subsequently be converted into histamine , which could be responsible for the effects of carnosine on neurotransmission and physiological function. Carnosine and its imidazole-containing dipeptide derivatives are renown with anti-aging, antioxidant, membrane protective, metal ion chelating , buffering, anti-glycation/ transglycating activities used to prevent and treat a spectrum of age-related and metabolic diseases, such as neurodegenerative disease, sight threatening eye diseases, Diabetes mellitus and its complications, cancers and other disorders due to their wide spectrum biological activities. The precursor of carnosine (and related imidazole containing compounds) synthesis in skeletal muscles beta-alanine is used as the oral supplement by athletes to achieve the fine sporting art results due to the buffering activities of carnosine and its related imidazole-containing compounds which contribute to maintenance of the acid-base balance in the acting muscles. This work originally emphasizes that overall data indicate on the signaling activities of carnosine in skeletal and cardiac muscles switching on the mechanisms of exercise-induced telomere protection and point to the stress response and growth/cellular proliferation pathways as high-priority candidates for the ongoing studies and therapeutic concepts. The therapeutic interventions utilizing the specific oral formulation (Can-C Plus), timing dosing and pharmaco-nutritional boost of imidazole-containing dipeptides can maintain health, enhance physical exercise performance and prevent aging. The patented therapeutic concept protects the existence of the interesting physiological major activities, better controls and therapeutic treatments for aging/age-related disorders (including age-related loss of muscle mass and muscle function) using carnosine dipeptide for cellular rejuvenation and manipulating telomeres and enzyme telomerase activity that may reduce some of the physiological declines that accompany aging.
    Recent Patents on Drug Delivery & Formulation 12/2014; 9(1). DOI:10.2174/1872211309666141218145408
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    ABSTRACT: Mucoadhesion began to be applied to therapeutic systems with the aim of the incorporation of bioadhesive molecules into pharmaceutical dosage forms intended to keep in close contact with the tissue, releasing the drug near the action site, thereby increasing its bioavailability and promoting local or systemic effects. Different mucoadhesive materials and dosage forms have been studied, since the properties of mucoadhesion largely depend on the features of the material used in its preparation. This mini-review focuses on mucoadhesive therapeutic systems, the main mucosal routes of administration, and materials used to prepare the systems over the last five years. Patents and applications were reviewed, categorized and the materials were described together with the proposed systems.
    Recent Patents on Drug Delivery & Formulation 11/2014; 9(1).
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    ABSTRACT: Recently, great attention has been paid to in situ gel-forming chitosan/glycerophosphate (CS/Gp) formulation due to its high biocompatibility with incorporated cells and medical agents, biodegradability and sharp thermosensitive gelation. CS/Gp is in liquid state at room temperature and after minimally invasive administration into the desired tissue, it forms a solid-like gel as a response to temperature increase. The overview of various recently patented strategies on injectable delivery systems indicates the significance of this formulation in biomedical applications. This thermosensitive hydrogel has a great potential as scaffold material in tissue engineering, due to its good biocompatibility, minimal immune reaction, high antibacterial nature, good adhesion to cells and the ability to be molded in various geometries. Moreover, CS/Gp hydrogel has been utilized as a smart drug delivery system to increase patient compliance by maintaining the drug level in the therapeutic window for a long time while avoiding the need for frequent injections of the therapeutic agent. This review paper highlights the recent investigations on different formulations of CS/Gp hydrogels as tissue engineering scaffolds and carriers for therapeutic agents. Additionally, the dominant mechanism of sol-gel transition in those systems as well as their physicochemical properties and biocompatibility are discussed in detail.
    Recent Patents on Drug Delivery & Formulation 10/2014; DOI:10.2174/1872211308666141028145651
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    ABSTRACT: Aims and Background: Donepezil (DNZ) is a centrally acting reversible acetyl cholinesterase inhibitor. The main therapeutic use of donepezil is in the treatment of Alzheimer's disease. The present research work pertains to the preparation of transdermal patches of donepezil with the objective to improve its patient compliance, therapeutic efficacy and to reduce the frequency of dosing and side effects as well as to avoid its extensive first pass metabolism. The recent patents on Rivastigmine (WO2013150542A2), Xanomeline (US5980933A) and Propentofylline (CA2255580A1) helped in selecting the drug and polymers. Materials and Methods: The transdermal patches were prepared using various polymers in combination with the plasticizer and penetration enhancers. The physicochemical parameters like folding endurance, thickness, drug content, content uniformity, moisture absorption, weight variation, and drug permeation studies of the optimized patches were studied. Results: The system containing Eudragit S -100, Eudragit E -100 and HPMC as matrix forming agent and glycerine as plasticizer was the best formulation. The in vitro release data was treated with kinetic equations and it followed zero order release. The diffusion study was carried out using rat skin showed 89% drug was released within 72 hours. Tween-80 (0.83 % w/w) was found to be the best among all penetration enhancers. All the transdermal patches had the desired physical properties like tensile strength, folding endurance, flatness and water vapor transmission rate etc. Conclusion: The study concluded that that transdermal patch can extend the release of donepezil for many hours and also ensure enhanced bioavailability, further it also helps in avoiding the first pass effect.
    Recent Patents on Drug Delivery & Formulation 10/2014; 9(1). DOI:10.2174/1872211308666141028213615
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    ABSTRACT: Nanoformulations (NF) are widely explored as a potential alternative for traditional ophthalmic formulation approaches. The effective treatment of ocular diseases using conventional eye drops is often hampered by factors such as: physiological barriers, rapid elimination, protein binding, and enzymatic drug degradation. Combined, these factors are known to contribute to reduced ocular residence time and poor bioavailability. Recent research studies demonstrated that NF can significantly enhance the therapeutic efficacy and bioavailability of ocular drugs, compared to the established ophthalmic drug delivery strategies. The research studies resulted in a number of patent inventions, reporting a significant increase in therapeutic efficacy for various chronic ocular disease states of both the anterior and posterior ocular segments. This article reviews these patent disclosures in detail and emphasizes on the therapeutic advantages conferred by the following nanoformulation approaches: "Calcium Phosphate (CaP) nanoparticles, Liposomes, Nanoemulsions, Nanomicelles, and Hydrogels". The nanoformulation approaches were shown to enhance the ocular bioavailability by reducing the drug-protein binding, increasing the corneal resident time, enhancing the drug permeability and providing a sustained drug release. Further, the article discusses United States Food and Drug Administration (USFDA) approved ocular drugs employing nanotechnology and future developments. It should be noted that, despite the potential therapeutic promise demonstrated by nanotechnology for ocular drug delivery, the bench to bed transition from patent inventions to marketed drug products has been insignificant. Majority of the discussed technologies are still in development and testing phase for commercial viability. Further, studies are in progress to assess ocular tolerance and nanotoxicity for prolonged use of NF.
    Recent Patents on Drug Delivery & Formulation 09/2014; DOI:10.2174/1872211308666140926112000
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    ABSTRACT: The much interest in the preparation (SEDDS) is to be a unique feasible approach to overcome low oral bioavailability problem and it is associated with the hydrophobic drugs due to their unparalleled potential as a drug delivery with the broad range of application. The estimated 40% of active pharmaceuticals are poorly water soluble. Now recently, formulation containing oral SEDDS has received much interest as a way to solve problems related to oral bioavailability, intra and inter-subject variability, lack of dose proportionality of hydrophobic drugs and now today it is the first way to investigated in the development of any kinds innovative dosage forms. Many important in-vitro characteristics such as surfactant concentration, oil/surfactant ratio, emulsion polarity, droplet size and zeta potential plays an important role in oral absorption of drug from SEEDS. It can be orally administered in the form of SGC or HGC and also enhance bioavailability of drugs to increase solubility and minimizes the gastric irritation. After administering the drug remains entrapped in the oily droplets (inside the droplet or in the surfactant`s film at the interface) of the emulsion that is being formed in the GIT upon self-emulsification process. It is also a bit problematic to say that the drug is being released from SMEDDS, it is more correct to say that it diffuses out of oily droplets into the GIT media and actually the equilibrium is formed between the drug dissolved in oily droplets and the outer dispersed media (e.g. GIT fluids). Many of the application and preparation method of SEDDS are reported by research articles and patents in different countries. We present an exhaustive and updated account of numerous literature reports and more than 150 patents published on SEDDS on recent period. We focused; this current patent review is useful in knowledge of SEDDS for its preparations and patents in different country with emphasis on their formulation, characterization and systematic optimization strategies, thus paving the way for accelerated progress into the SEDDS application in pharmaceutical research as well as patents on SEDDS methods.
    Recent Patents on Drug Delivery & Formulation 08/2014; DOI:10.2174/1872211308666140821120203
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    ABSTRACT: Eye inflammation, if untreated at right time poses the risk of vision loss. Several categories of drugs are available in the global market, but corticosteroids are still used for the treatment of ocular inflammation including anterior/posterior uveitis, age related macular degeneration (AMD) and post cataract surgery inflammation. Although corticosteroids have well-documented side effects as compared to non steroidal anti-inflammatory drugs (NSAIDs), but they are still regarded as better anti-inflammatory agents for treating ocular inflammations. The prime concern with conventional formulations such as (ophthalmic solutions, suspensions, ointments) is low drug bioavailability due to precorneal barrier of the eye, tear turnover and rapid drainage of drug via nasolacrimal drainage and drug induced systemic toxicity. To overcome these limitations, various novel formulations of corticosteroids have been explored. These include nanoparticles, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), nanomicelles, in-situ gels, iontophoresis, liposomes, nanoemulsions, microemulsions and ocular implants for the effective ophthalmic delivery of the corticosteroids. Topical nanocarriers have also been demonstrated to be promising vectors with potential application in the ophthalmic therapeutics. This review summarizes the clinical findings and patents on various corticosteroids as ocular pharmacotherapeutics.
    Recent Patents on Drug Delivery & Formulation 07/2014; DOI:10.2174/1872211308666140713171702
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    ABSTRACT: Oral administration of Insulin, however, is extremely difficult due to their extremely low bioavailability. Development of oral Insulin formulations requires overcoming obstacles, such as low permeability of large molecules, lack of lipophilicity, and inactivation or rapid enzymatic degradation in the gastrointestinal (GI) tract. The successful oral delivery of Insulin involves overcoming the barrier of enzymatic degradation, achieving epithelial permeability, and conserving the bioactivity of the drug during formulation processing. Strategies proposed to maximize oral Insulin bioavailability in Insulin delivery systems, to overcome barriers, and to develop safe and effective therapies, by using specific excipients, such as absorption enhancers, enzyme inhibitors, and mucoadhesive polymers, and using composition allowing protection of Insulin from the harsh environment in the GI tract. The present review includes study of patents on oral Insulin delivery. All the patents in the present review are arranged and interconnected in such a way to improve viewer's knowledge at glance. The comparative comments and discussions on the entitled topic make it easier to understand.
    Recent Patents on Drug Delivery & Formulation 06/2014; DOI:10.2174/1872211308666140701093351
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    ABSTRACT: The present critical review is related with the self modified patch based drug delivery system for controlled (trans)dermal drug delivery. The composition itself modified into the patch and adheres when comes onto the skin contact and acts as a rate-controlling matrix layer (patch). The self adhesiveness property of the formulation itself is enough to hold the patch in place on the skin for the encouraged duration of treatment while allowing the patch to be promptly backed away without any skin irritation and formulation residue. This patent review is useful in knowledge of self modified patch associated drug delivery for controlled topical or transdermal delivery of pharmaceutical and cosmetic agents.
    Recent Patents on Drug Delivery & Formulation 06/2014; 9(1). DOI:10.2174/187221130901150303113918
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    ABSTRACT: It has been documented that telomere-associated cellular senescence may contribute to certain age-related disorders, including an increase in cancer incidence, wrinkling and diminished skin elasticity, atherosclerosis, osteoporosis, weight loss, age-related cataract, glaucoma and others. Shorter telomere length in leukocytes was associated cross-sectionally with cardiovascular disorders and its risk factors, including pulse pressure and vascular aging, obesity, vascular dementia, diabetes, coronary artery disease, myocardial infarction (although not in all studies), cellular turnover and exposure to oxidative and inflammatory damage in chronic obstructive pulmonary disease . It has been proposed that telomere length may not be a strong biomarker of survival in older individuals, but it may be an informative biomarker of healthy aging. The data reveal that telomere dynamics and changes in telomerase activity are consistent elements of cellular alterations associated with changes in proliferative state and in this article these processes are consequently considered as the new therapeutic drug targets for physiological control with advanced drug delivery and nutritional formulations. In particular, the presence of highly specific correlations and early causal relationships between telomere loss in the absence of telomerase activity and replicative senescence or crisis, and from the other side, telomerase reactivation and cell immortality, point to a new and important treatment strategies or the therapeutic manipulation during treatment of age related disorders and cancer. Once better controls and therapeutic treatments for aging and age-related disorders are achieved, cellular rejuvenation by manipulating telomeres and enzyme telomerase activity may reduce some of the physiological declines that accompany aging. In this work we raise and support a therapeutic concept of using non-hydrolized forms of naturally occurring imidazole-dipeptide based compounds carnosine and carcinine, making it clinically possible that slowing down the rate of telomere shortening could slow down the human aging process in specific tissues where proliferative senescence is known to occur with the demonstrated evidence of telomere shortening appeared to be a hallmark of oxidative stress and disease. The preliminary longitudinal studies of elderly individuals suggest that longer telomeres are associated with better survival and an advanced oral nutritional support with non-hydrolized carnosine (or carcinine and patented compositions thereof) is a useful therapeutic tool of a critical telomere length maintenance that may fundamentally be applied in the treatment of age-related sight-threatenting eye disorders, prolong life expectancy, increase survival and chronological age of an organism in health control, smoking behavior and disease.
    Recent Patents on Drug Delivery & Formulation 06/2014; 8(3). DOI:10.2174/1872211308666140602125505
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    ABSTRACT: Insulin was discovered over 90 years ago. From then till now oral insulin is still a challenging and elusive goal. However huge efforts are being done worldwide for developing noninvasive drug delivery systems, mainly via oral route as it is the most widely accepted means of administration. The main barriers faced in oral protein delivery are the enzymatic degradation and poor permeability across the intestinal wall. All the approaches for oral insulin are on how to overcome these barriers. To overcome the gastro-intestinal barriers various types of formulations such as insulin conjugates, permeation enhancers, micro/nanoparticles, liposomes etc. are investigated. In the recent years lot of advances have taken place in understanding of the oral peptide delivery systems. In this review the recent patents on oral insulin is focused. Emphasis is on the technologies based on permeation enhancers and nanoparticle based carrier systems.
    Recent Patents on Drug Delivery & Formulation 05/2014; DOI:10.2174/1872211308666140527143407